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A potent TGR5(GPCR19) agonist that showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). Synonyms: TGR5; TGR 5; TGR-5; TGR5 Receptor Agonist; MDK00245; MDK-00245; MDK 00245. CAS No. 1197300-24-5. Molecular formula: C18H14Cl2N2O2. Mole weight: 361.222.
TGR5 Receptor Agonist
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC 50 s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity [1] [2] [3] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CCDC. CAS No. 1197300-24-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-14229.
Cell-permeable, small molecule agonist of TGR5 G-protein coupled receptor. This agonist has shown to increase glucagon like peptide-1 (GLP-1) secretion from primary intestinal cells. Group: Biochemicals. Alternative Names: 3-(2-Chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethylisoxazole-4-carboxamide. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
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TGR5 Receptor Agonist, Cpd23g ( (4-cyclopropyl-3, 4-dihydroquinoxalin-1 (2H) -yl) (4- (2, 5-dimethylphenoxy) pyridin-3-yl) methanone, Bile Acid Receptor GPBAR-1 Agonist, Bile Acid Receptor Agonist, G Protein-coupled Bile Acid Receptor 1 Agonist)
A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM and 6.2nM for human and mouse TGR5, respectively). Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120. Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t½ = 1.5h, Cmax = 56ng/ml; and AUC = 147ng.h/ml following an oral dose of 5mg/kg). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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Betulinic Acid
Betulinic Acid is a natural pentacyclic triterpenoid. Betulinic Acid displays anti-inflammatory and anti-HIV activity. Betulinic Acid selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic Acid also exhibits TGR5 agonist activity. Group: Biochemicals. Alternative Names: Mairin; (+)-Betulinic acid; 3 β-Hydroxylup-20(29)-en-28-oic Acid; Betulic Acid; Lupatic Acid; NSC 113090; β-Betulinic Acid; (3 β)-3-HydroxyLup-20(29)-en-28-oic Acid. Grades: Highly Purified. CAS No. 472-15-1. Pack Sizes: 100mg, 250mg, 500mg. Molecular Formula: C??H??O?, Molecular Weight: 456.7. US Biological Life Sciences.
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Cholic acid 7-sulfate
Cholic acid 7-sulfate (7-Sulfocholic acid), a metabolite of Cholic acid, is a Takeda G-protein receptor 5 (TGR5) agonist. Cholic acid 7-sulfate can increase Tgr5 expression and induce GLP-1 secretion [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 7-Sulfocholic acid. CAS No. 60320-05-0. Pack Sizes: 500 μg; 1 mg; 5 mg. Product ID: HY-126855.
Cloxacillin EP Impurity D
3-(2-Chlorophenyl)-5-methylisoxazole-4-carboxylic Acid is used in the preparation of isoxazolecarboxamides as a class of TGR5 agonists. It is also used in the preparation of β-lactamase inhibitors. Synonyms: 3-(2-Chlorophenyl)-5-methylisoxazole-4-carboxylic Acid. Grades: > 95%. CAS No. 23598-72-3. Molecular formula: C11H8ClNO3. Mole weight: 237.64.
Deoxycholic acid
Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptor TGR5 [1] [2]. Uses: Scientific research. Group: Natural products. Alternative Names: Cholanoic Acid; Desoxycholic acid. CAS No. 83-44-3. Pack Sizes: 10 mM * 1 mL; 100 mg; 500 mg. Product ID: HY-N0593.
Deoxycholic acid
Deoxycholic acid is one of the secondary bile acids, which are metabolic byproducts of intestinal bacteria. Deoxycholic acid is specifically responsible for activating the G-protein-coupled bile acid receptor TGR5, stimulating the thermogenic activity of brown adipose tissue (BAT). Uses: Hypotensive. Synonyms: Cholanoic Acid; Desoxycholic acid; 3α,12α-dihydroxy-5β-cholanate; Deoxycholate; Cholerebic; Degalol; Droxolan; Pyrochol; 5β-cholanic acid-3α,12α-diol; 7-Deoxycholic acid; 5β-Deoxycholic Acid; NSC 8797; Septocholl; Ursodeoxycholic Acid EP Impurity E. Grades: >98%. CAS No. 83-44-3. Molecular formula: C24H40O4. Mole weight: 392.58.
Deoxycholic acid sodium salt
Deoxycholic acid sodium salt (sodium deoxycholate), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptor TGR5 [1] [2]. Uses: Scientific research. Group: Natural products. Alternative Names: Sodium deoxycholate. CAS No. 302-95-4. Pack Sizes: 100 mg; 500 mg. Product ID: HY-N0593A.
EP-024297
EP-024297 is a novel agonist of farnesoid X receptor (FXR). Study in Chinese hamster ovary cells showed that it is 20000-fold more potent than obeticholic acid (OCA). EP-024297 is selective for FXR over TGR5. It promisingly becomes a new treatment of NASH. Uses: The potential treatment of nash. Synonyms: EP-024297; EP 024297; EP024297.
Hyocholic Acid
Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. CAS No. 547-75-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-121238.
Hyodeoxycholic acid
Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC 50 of 31.6 μM in CHO cells. Uses: Scientific research. Group: Natural products. Alternative Names: HDCA. CAS No. 83-49-8. Pack Sizes: 10 mM * 1 mL; 100 mg; 500 mg. Product ID: HY-N0169.
Hyodeoxycholic acid (HDCA)
Hyodeoxycholic acid is a secondary bile acid, one of the metabolic byproducts of intestinal bacteria. It is a TGR5 (GPCR19) agonist, with an EC50 of 31.6 μM in CHO cells. Synonyms: Iodeoxycholic acid; 7-Deoxyhyocholic acid; 3α,6α-Dihydroxy-5β-cholan-24-oic acid; 5β-cholan-24-oic acid-3α,6α-Diol; α-Hyodeoxycholic acid; 3α,6α-Dihydroxy-5β-cholanic acid. Grades: >98%. CAS No. 83-49-8. Molecular formula: C24H40O4. Mole weight: 392.57.
INT-767
INT-767, a steride compound, has been found to be a inhibitor of FXR and TGF5 and could have probable effect against some liver and metabolic diseases. It was just planed a Phase II trial for Hepatic fibrosis. IC50: 30 nM(EC50, FXR), 630 nM(EC50, TGR5). Uses: Int-767 has been found to be a inhibitor of fxr and tgf5 and could have probable effect against some liver and metabolic diseases. Synonyms: INT-767; INT 767; INT767; CS-5007; CS 5007; CS5007; HY-12434; HY 12434; HY12434; Sulfuric acid sodium 3alpha,7alpha-dihydroxy-6alpha-ethyl-24-nor-5beta-cholane-23-yl ester salt. Grades: 98%. CAS No. 1000403-03-1. Molecular formula: C25H43NaO6S. Mole weight: 494.66.
INT-777
INT-777(S-EMCA) is a novel potent and selective TGR5 agonist with remarkable in vivo activity (EC50=0.82 uM). Synonyms: INT-777; INT 777; INT777; 6-EMCA; S-EMCA; ?HY-15677. Grades: >98%. CAS No. 1199796-29-6. Molecular formula: C27H46O5. Mole weight: 450.65.
Lithocholic Acid
A cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: (3α,5 β)-3-Hydroxycholan-24-oic Acid; 17 β - (1-Methyl-3-carboxypropyl) etiocholan-3α -ol; 3-Hydroxycholan-24-oic Acid; 3α-Hydroxy-5 β-cholan-24-oate; 3α-Hydroxy-5 β-cholan-24-oic Acid; 3α-Hydroxy-5 β-cholanic Acid; 3α-Hydroxy-5 β-cholanoic Acid; 3α-Hydroxycholanic Acid; NSC 683770. Grades: Highly Purified. CAS No. 434-13-9. Pack Sizes: 1g. US Biological Life Sciences.
Worldwide
Lithocholic Acid
A cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 3α-Hydroxy-5β-cholanic acid. Product Category: Steroidal Compounds. Appearance: White to off-white powder. CAS No. 434-13-9. Molecular formula: C24H40O3. Mole weight: 376.57. Purity: 0.98. IUPACName: (4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid. Canonical SMILES: CC(CCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C. Density: 1.0454 g/cm³. ECNumber: 207-099-1. Product ID: ACM434139. Alfa Chemistry ISO 9001:2015 Certified.
Lithocholic Acid 24-Ac-O-β-D-Glucuronide
Lithocholic Acid 24-Ac-O-β-D-Glucuronide is an impurity of Lithocholic Acid (L469180), a cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Synonyms: 1-[(3α,5β)-3-Hydroxycholan-24-oate] β-D-Glucopyranuronic Acid. CAS No. 142780-61-8. Molecular formula: C30H48O9. Mole weight: 552.7.
Lithocholic Acid 3-O-Glucuronide
Lithocholic Acid 3-O-Glucuronide is an impurity of Lithocholic Acid, a cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Synonyms: (3α,5β)-23-Carboxy-24-norcholan-3-yl β-D-Glucopyranosiduronic Acid; Lithocholic Acid 3-Glucuronide. Grades: 98%. CAS No. 75239-91-7. Molecular formula: C30H48O9. Mole weight: 552.7.
Lithocholic Acid-d4
A labeled cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: (3α,5 β)-3-Hydroxycholan-24-oic Acid-d4; 17 β - (1-Methyl-3-carboxypropyl) etiocholan-3α -ol-d4; 3-Hydroxycholan-24-oic Acid-d4; 3α-Hydroxy-5 β-cholan-24-oate-d4; 3α-Hydroxy-5 β-cholan-24-oic Acid-d4; 3α-Hydroxy-5 β-cholanic Acid-d4; 3α-Hydroxy-5 β-cholanoic Acid-d4; 3α-Hydroxycholanic Acid-d4; NSC 683770-d4. Grades: Highly Purified. CAS No. 83701-16-0. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Lithocholic Acid-d5
A labelled cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: (3α,5 β)-3-Hydroxycholan-24-oic Acid-d5; 17 β - (1-Methyl-3-carboxypropyl) etiocholan-3α -ol-d5; 3-Hydroxycholan-24-oic Acid-d5; 3α-Hydroxy-5 β-cholan-24-oate-d5; 3α-Hydroxy-5 β-cholan-24-oic Acid-d5; 3α-Hydroxy-5 β-cholanic Acid-d5; 3α-Hydroxy-5 β-cholanoic Acid-d5; 3α-Hydroxycholanic Acid-d5; NSC 683770-d5. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Methyl Isolithocholate-d7
Methyl Isolithocholate-d7 is a labelled cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: Methyl 3 β-Hydroxy-5 β-cholanoate; 3 β-Hydroxy-5 β-cholanic Acid Methyl Ester-d7; (3 β,5 β)-3-Hydroxycholan-24-oic Acid Methyl Ester-d7. Grades: Highly Purified. CAS No. 5405-42-5. Pack Sizes: 2.5mg. US Biological Life Sciences.
Worldwide
Methyl Lithocholate
Methyl Lithocholate is an derivative of Lithocholic Acid (L469180),a cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: Lithocholic Acid Methyl Ester-d7; Methyl 3α-Hydroxy-5 β-cholan-24-oate-d7; Methyl 3α-Hydroxy-5 β-cholanoate-d7; 3α-Hydroxy-5 β-cholanic Acid-d7; 3α-Hydroxy-5 β-cholan-24-oic Acid Methyl Ester-d7; (3α,5 β)-3-Hydroxycholan-24-oic Acid Methyl Ester-d7. Grades: Highly Purified. CAS No. 1249-75-8. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
Methyl Lithocholate-d7
Isotope labelled derivative of Lithocholic Acid (L469180),a cholic acid derivative as TGR5 modulator. Found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: Lithocholic Acid Methyl Ester-d7; Methyl 3α-Hydroxy-5 β-cholan-24-oate-d7; Methyl 3α-Hydroxy-5 β-cholanoate-d7; 3α-Hydroxy-5 β-cholanic Acid-d7; 3α-Hydroxy-5 β-cholan-24-oic Acid Methyl Ester-d7; (3α,5 β)-3-Hydroxycholan-24-oic Acid Methyl Ester-d7. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Milbemycin oxime
Milbemycin oxime is a semi-synthetic macrolide. As a nematocide and insecticide in veterinary medicine, it opens glutamate sensitive chloride channels in neurons of invertebrates that leads to paralysis by hyperpolarisation of these cells and signal transfer blocking. M1-family aminopeptidase: IC50=2.6 μM (Plasmodium falciparum 3D7); Bile acid transporter: IC50=3.6 μM (human); TGR5: IC50=36.4 μM (human); HCT-116: IC50 >50 μM (human); GBM: IC50 >50 μM (human). Uses: A broad spectrum insecticide; used for treatment and prevention of heartworm in dogs and cats. Synonyms: Milbemycin A 5-oxime; Milbemite; Trifexis; Interceptor; Milbe Mite. Grades: ≥98%. CAS No. 129496-10-2. Molecular formula: C126H176N4O28. Mole weight: 2194.78.
SB756050
SB756050 is a selective TGR5 agonist currently undergone testing in a phase 1 clinical trials study in the treatment of type 2 diabetes. Synonyms: 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]-1,4-diazepane; SB756050; F1018-1711; 1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane; SB-756050; SB 756050; SB756050. CAS No. 447410-57-3. Molecular formula: C21H28N2O8S2. Mole weight: 500.59.
Sulfolithocholic Acid Trimethylamine Salt
Sulfolithocholic Acid is an derivative of Lithocholic Acid (L469180), a cholic acid derivative and TGR5 modulator found in ox bile, human bile, rabbit bile, and in ox and pig gallstones. Group: Biochemicals. Alternative Names: 3α-Sulfate-5 β-cholan-24-oic Acid Trimethylamine Salt; Lithocholic Acid 3-O-Sulfate Trimethylamine Salt ; Lithocholic Acid 3α-Sulfate Trimethylamine Salt; (3α,5 β)-3-(Sulfooxy)-cholan-24-oic Acid Trimethylamine Salt. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
Taurodeoxycholic acid sodium hydrate
Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. Taurodeoxycholic acid sodium hydrate activates the S1PR2 pathway in addition to the TGR5 pathway [1]. Uses: Scientific research. Group: Natural products. Alternative Names: Sodium taurodeoxycholate monohydrate. CAS No. 110026-03-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-B1899A.
TC-G 1005
TC-G 1005 is a potent and selective GPBA agonist (EC50 = 0.72 nM for hTGR5) that selectively activates TGR5 over FXR (farnesoid X receptor). TC-G 1005 has been shown to increase plasma GLP-1 level and lower blood glucose level in mice. Synonyms: TC-G 1005; TC G 1005; TCG 1005; TC-G-1005; TCG1005; (4-Cyclopropyl-3,4-dihydro-1(2H)-quinoxalinyl)[4-(2,5-dimethylphenoxy)-3-pyridinyl]methanone. Grades: ≥98% by HPLC. CAS No. 1415407-60-1. Molecular formula: C25H25N3O2. Mole weight: 399.48.
Triamterene
Triamterene blocks epithelial Na + channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene is an inhibitor of the TGR5 receptor [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 396-01-0. Pack Sizes: 10 mM * 1 mL; 100 mg; 500 mg. Product ID: HY-B0575.
Triamterene (Standard)
Triamterene (Standard) is the analytical standard of Triamterene. This product is intended for research and analytical applications. Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor. Uses: Scientific research. Group: Signaling pathways. CAS No. 396-01-0. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-B0575R.
Ursodeoxycholic acid
Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 ( TGR5 , GPCR19 ) and the farnesoid X receptor ( FXR ). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. Alternative Names: Ursodeoxycholate; Ursodiol; UDCA. CAS No. 128-13-2. Pack Sizes: 10 mM * 1 mL; 1 g; 5 g. Product ID: HY-13771.
Ursodeoxycholic acid-2,2,4,4-d4
Ursodeoxycholic acid-2,2,4,4-d 4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection[1][2][3][4][5]. Uses: Scientific research. Group: Isotope-labeled compounds. CAS No. 347841-46-7. Pack Sizes: 500 μg; 1 mg; 5 mg. Product ID: HY-113478S.
Ursodeoxycholic acid sodium
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 ( TGR5 , GPCR19 ) and the farnesoid X receptor ( FXR ). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active [1] [2]. Uses: Scientific research. Group: Natural products. Alternative Names: Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium. CAS No. 2898-95-5. Pack Sizes: 10 mM * 1 mL; 50 mg; 100 mg; 500 mg; 1 g; 5 g. Product ID: HY-13771A.
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