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Orexin receptor antagonist 2 (compound 30) is a potent orexin receptor antagonist with pK i s of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1457940-75-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-136922.
Orexin receptor antagonist 3
Orexin receptor antagonist 3 (example 216) is an orexin receptor antagonist, which is extracted from the patent WO2011050198A1 [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1293282-55-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-137093.
1-(tert-Butyloxycarbonyl)-3,3-difluoro-4-aminopiperidine is synthetic building block for pharmaceuticals. It can be obtained from N-Benzyl- β-alanine Ethyl Ester (B232975) which is used as a reagent in organic synthesis including that of dipivaloyloxyphenyl aminopropionate β-agonist prodrugs which are used in the treatment of psoriasis. N-Benzyl- β-alanine Ethyl Ester (B232975) is also used in the synthesis of N,N'-dithiobis(N-benzyl- β-alanine) dethyl ester, which is an important intermediate of insecticide OK-135, and in synthesis of spiropiperidine-based orexin-2 receptor (OX2R) antagonists. Group: Biochemicals. Grades: Highly Purified. CAS No. 1255666-48-8. Pack Sizes: 100mg, 500mg. Molecular Formula: C10H18F2N2O2, Molecular Weight: 236.26. US Biological Life Sciences.
Worldwide
2-Acetyl-4- (trifluoromethyl) phenol
2-Acetyl-4- (trifluoromethyl) phenol was used to study benzoxazepine-?based Orexin-?2 receptor antagonists. Group: Biochemicals. Grades: Highly Purified. CAS No. 67589-15-5. Pack Sizes: 50mg, 100mg. Molecular Formula: C9H7F3O2, Molecular Weight: 204.15. US Biological Life Sciences.
Worldwide
2-Amino-5-fluoronicotinic acid
2-Amino-5-fluoronicotinic Acid acts as a reagent used in the synthesis of fluoropiperidine derivatives as orexin receptor antagonists. Group: Biochemicals. Grades: Highly Purified. CAS No. 1196154-03-6. Pack Sizes: 10mg, 25mg. Molecular Formula: C6H5FN2O2, Molecular Weight: 156.12. US Biological Life Sciences.
Worldwide
2-Methyl-1,3-benzoxazole-6-carboxylic Acid
2-Methyl-1,3-benzoxazole-6-carboxylic Acid is used in the synthesis of orexin 1 receptor antagonists, used in the treatment of obesity. Also used in the synthesis of novel benzoxazole amides as novel enhancers of HIV-1 protease inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 13452-14-7. Pack Sizes: 100mg, 500 mg. Molecular Formula: C9H7NO3. US Biological Life Sciences.
(2R,5R)-Benzyl 5-amino-2-methylpiperidine-1-carboxylate is a reactant used in the preparation of pyridylamino-nitrile-piperidinyl Orexin receptor antagonists. Group: Biochemicals. Grades: Highly Purified. CAS No. 1207853-72-2. Pack Sizes: 2.5mg, 25mg. Molecular Formula: C14H20N2O2, Molecular Weight: 248.32. US Biological Life Sciences.
Worldwide
ACT 335827
ACT 335827 has been found to be an orexin OX1 receptor antagonist and could probably exhibit anxiolytic effects in vivo. Synonyms: ACT-335827; ACT 335827; ACT335827; (aR,1S)-1-[(3,4-Dimethoxyphenyl)methyl]-3,4-dihydro-6,7-dimethoxy-N-(1-methylethyl)-a-phenyl-2(1H)-isoquinolineacetamide. Grades: ≥98% by HPLC. CAS No. 1354039-86-3. Molecular formula: C31H38N2O5. Mole weight: 518.64.
ACT 462206
ACT 462206 has been found to be a potent and selective dual orexin receptor antagonist and could exhibit anxiolytic-like activities. Synonyms: ACT-462206; ACT 462206; ACT462206; (2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide. Grades: ≥99% by HPLC. CAS No. 1361321-96-1. Molecular formula: C20H24N2O4S. Mole weight: 388.48.
ACT-462206
ACT-462206 is an orally active and potent dual Orexin 1 / Orexin 2 receptor antagonist with IC 50 s of 60 nM ( Orexin 1 ) and 11 nM ( Orexin 2 ), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1361321-96-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-101834.
Almorexant
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with K d values of 1.3 nM ( OX1 ) and 0.17 nM ( OX2 ), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis [1] [2] [3] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ACT 078573. CAS No. 871224-64-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10805.
Almorexant
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. Uses: For research used only. Synonyms: ACT-078573. Grades: 0.99. CAS No. 871224-64-5. Molecular formula: C29H31F3N2O3. Mole weight: 512.573.
Almorexant HCl
Almorexant HCl is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. Synonyms: ACT078573; ACT 078573; ACT-078573. Grades: >98%. CAS No. 913358-93-7. Molecular formula: C29H32ClF3N2O3. Mole weight: 549.02.
Almorexant hydrochloride
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with K d values of 1.3 nM ( OX1 ) and 0.17 nM ( OX2 ), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis [1] [2] [3] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ACT 078573 hydrochloride. CAS No. 913358-93-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10805A.
EMPA
EMPA is a high-affinity, reversible and selective orexin OX 2 receptor antagonist. [ 3 H]EMPA binds to human and rat OX 2 -HEK293 membranes with K D values of 1.1 and 1.4 nM respectively [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 680590-49-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-108682.
EMPA
EMPA is a potent and selective OX2 receptor antagonist (IC50 = 2.3 nM and 1900 nM for OX2 and OX1, respectively) with no activity at a panel of 80 receptors. EMPA blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX2-expressing CHO cells (IC50 = 7.9 nM and 8.8 nM, respectively) and reverses orexin-B-induced hyperlocomotion in mice. Synonyms: N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide. Grades: ≥98% by HPLC. CAS No. 680590-49-2. Molecular formula: C23H26N4O4S. Mole weight: 454.54.
JNJ-10397049
JNJ-10397049 is a potent and selective orexin 2 receptor (OX 2 R) antagonist, with a pK i of 8.3. JNJ-10397049 is 600-fold selective for the OX 2 R over the OX 1 R [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 708275-58-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10896.
JNJ-10397049
JNJ-10397049 is a selective orexin-2 receptor (OX2) antagonist. pIC50 is 7.4 for chimeric OX2 receptors/ pKB values are 5.9 for OX1 and 8.5 for OX2 receptors respectively. JNJ-10397049 exhibits no significant activity in a panel of over 50 other neurotransmitters and neuropeptide receptors. It achieves high level of OX2 receptor occupancy in the rat brain. Synonyms: JNJ-10397049; JNJ 10397049; JNJ10397049; 1-(2,4-Dibromophenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-(1,3)dioxan-5-yl)urea. Grades: 98%. CAS No. 708275-58-5. Molecular formula: C19H20Br2N2O3. Mole weight: 484.19.
Mk1064
Mk1064 is a selective orexin OX2 receptor antagonist for potential treatment of insomnia. Studies shows that Mk1064 could promote sleep and increase both rapid eye movement (REM) and non-REM (NREM) sleep of humans. Uses: Mk1064 is a selective orexin ox2 receptor antagonist. Synonyms: MK1064; MK 1064; MK-1064; 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide. Grades: ≥98%. CAS No. 1207253-08-4. Molecular formula: C24H20ClN5O3. Mole weight: 461.91.
MK-3697
MK3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. MK-3697 is also the third insomnia product, currently being developed by Merck. MK-3697 has Ki = 0.95 nM. Orexin receptor antagonists have demonstrated clinical utility for the treatment of insomnia. In vivo tests results on MK-3697 demonstrated improved stability and TDI profiles as well as excellent sleep efficacy across species. Synonyms: MK-3697; MK3697; MK 3697. Grades: 0.99. CAS No. 1224846-01-8. Molecular formula: C23H21N5O3S. Mole weight: 447.513.
Nalfurafine (TRK-820)
Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05nM for human receptors expressed in CHO cell membranes).1 It is selective for κ-opioid over μ- and δ-opioid receptors (EC50s = 0.72 and 74.1nM, respectively). Nalfurafine (≥30ug/kg) reduces scratching behavior induced by chloroquine in mice, as well as locomotor activity when administered at a dose of 100ug/kg.2 In rats, nalfurafine (≥0.01mg/kg) reduces intracranial self-stimulation, lactic acid-induced stretching behavior, and scratching behavior induced by intradermal administration of serotonin.3 Nalfurafine is also an orexin 1 receptor (OX1R) antagonist (Ki = 250nM).4. Group: Biochemicals. Alternative Names: (2E)-N-[(5α,6 β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide; TRK-820. Grades: Highly Purified. CAS No. 152657-84-6. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C28H32N2O5, Molecular Weight: 476.56. US Biological Life Sciences.
Worldwide
Nivasorexant
Nivasorexant is a potent orexin receptor antagonist [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ACT-539313. CAS No. 1435480-40-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-147294.
SB-334867
SB-334867 (SB 334867A) is an excellent,selective and blood - brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 ( pK b =7.4), 100-fold over 5-HT 2B , 5-HT 2C with pK i values of 5.4 and 5.3, respectively [1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SB 334867A. CAS No. 249889-64-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10895.
SB-334867
SB-334867, with sedative and anorectic effects, it is the first non-peptide selective antagonist of orexin receptor subtype OX1 (pKb= 7.2) with 50 -fold selectivity for OX1 over OX2 receptors. in vitro: inhibited the orexin-A (10 nM) and orexin-B (100 nM). Synonyms: 1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea 1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea 1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea hydrochloride SB 334867-A SB 334867A SB-334867 SB-334867-A SB-334867A SB3348. Grades: >99 %. CAS No. 249889-64-3. Molecular formula: C17H13N5O2. Mole weight: 319.32.
SB-334867 free base
SB-334867 free base (SB334867A free base) is an excellent, selective and blood - brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 ( pK b =7.4), 100-fold over 5-HT 2B , 5-HT 2C with pK i values of 5.4 and 5.3, respectively [1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SB334867A free base. CAS No. 792173-99-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10895A.
SB-408124 Hydrochloride
SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with K i s of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1431697-90-3. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-76612.
SB-649868
SB-649868 is a novel, orally active dual orexin receptor antagonist of orexin(OX)1 and OX2 receptor (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively), potentially for the treatment of insomnia and sleep disorder. Synonyms: N-[[(2S)-1-[5-(4-fluorophenyl)-2-methyl-1,3-thiazole-4-carbonyl]piperidin-2-yl]methyl]-1-benzofuran-4-carboxamide; (14C)SB 649868; (14C)SB-649868; (14C)SB649868; N-((1-((5-(4-fluorophenyl)-2-methyl-4-thiazolyl)carbonyl)-2-piperidinyl)methyl)-4-benzofurancarboxamide; SB 649868; SB-649868; SB649868; GSK-649868; GSK-649868; GSK649868. CAS No. 380899-24-1. Molecular formula: C26H24FN3O3S. Mole weight: 477.55.
SB-649868
SB-649868 is a potent and selective orally active orexin ( OX ) 1 and OX 2 receptor antagonist ( pK i =9.4 and 9.5 at the OX 1 and OX 2 receptor, respectively). Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSK649868. CAS No. 380899-24-1. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10806.
SB-674042
SB-674042 is a potent and selective non-peptide orexin OX 1 receptor antagonist (K d =5.03 nM), exhibits 100-fold selectivity for OX 1 over OX 2 receptors with IC 50 values of 3.76 nM and 531 nM, respectively [1] [4]. Uses: Scientific research. Group: Signaling pathways. CAS No. 483313-22-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10898.
SB-674042
SB-674042 is potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM), by binding with high affinity to OX1R and mediates intracellular calcium flux in OX1R-expressing cells. Uses: Potent and selective non-peptide orexin ox1 receptor antagonist. Synonyms: SB 674042; SB-674042; SB674042; [5-(2-Fluorophenyl)-2-methyl-4-thiazolyl][2(S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl-1-pyrrolidinyl]methanone. Grades: ≥98%. CAS No. 483313-22-0. Molecular formula: C24H21FN4O2S. Mole weight: 448.51.
Seltorexant
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist ( pK i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: JNJ-42847922. CAS No. 1293281-49-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-109012.
TCS 1102
TCS 1102 is a potent, dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively. It is a poor substrate for P-glycoprotein, which demonstrates good brain penetration when administered intraperitoneally. It were found to decrease fear and anxiety in rats 14 days after exposure to footshock. It was also found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze. Uses: Tcs 1102 was found to have anxiolytic effects. Synonyms: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide;2-PyrrolidinecarboxaMide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-Methyl-1H-benziMidazol-2-yl)thio]acetyl]-, (2S)-;(2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide;TCS 1102, TCS1102, TCS-1102;(2S)-1-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-N-(2-phenylphenyl)pyrrolidine-2-carboxamide. Grades: >98 %. CAS No. 916141-36-1. Molecular formula: C27H26N4O2S. Mole weight: 470.59.
TCS OX2 29
TCS OX2 29 is a potent and selective OX2 receptor antagonist (IC50 = 40 nM) displaying >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Orexin is a neuropeptide produced in the lateral hypothalamus (LH) regulates arousal, pain and appetite. Synonyms: (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride. Grades: ≥98% by HPLC. CAS No. 372523-75-6. Molecular formula: C23H31N3O3.HCl. Mole weight: 433.97.
TCS-OX2-29
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX 2 R) antagonist with an IC 50 value of 40 nM and a pK I value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX 2 over OX 1 [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 372523-75-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100452.
Vornorexant
Vornorexant is a new and powerful dual orexin 1/2 receptor (OX1/2R) antagonist for the treatment of insomnia. Synonyms: (-)-[2-[[3-(5-Fluoropyridin-2-yl)-1H-pyrazol-1-yl]methyl]-1,3-oxazinan-3-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone. Grades: >98%. CAS No. 2265899-49-6. Molecular formula: C23H22FN7O2. Mole weight: 447.5.
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