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Nociceptin, a 17 amino acid neuropeptide involved in a variety of biological systems, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Synonyms: Orphanin FQ; H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln-OH; L-phenylalanyl-glycyl-glycyl-L-phenylalanyl-L-threonyl-glycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-alanyl-L-asparagyl-L-glutamine; Nociceptin/orphanin FQ; Nociceptin (1-17); Orphanin FQ (rat, human, swine). Grades: ≥98% by HPLC. CAS No. 170713-75-4. Molecular formula: C79H129N27O22. Mole weight: 1809.04.
Nociceptin
Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Uses: Scientific research. Group: Peptides. Alternative Names: Orphanin FQ. CAS No. 170713-75-4. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-P0183.
Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes. Synonyms: H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-NH2.TFA; L-phenylalanyl-glycyl-glycyl-L-phenylalanyl-L-threonyl-glycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysinamide trifluoroacetic acid. Grades: 99%. Molecular formula: C63H101F3N22O17. Mole weight: 1495.61.
Nociceptin (1-7)
Nociceptin (1-7), the N-terminal fragment of Nociceptin, antagonizes nociceptin-induced hyperalgesia, with no effect on nociceptin-induced analgesia. Synonyms: L-Phenylalanylglycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanine; 1-7-Orphanin FQ (pig); (2S) -2- [ [2- [ [ (2S, 3R) -2- [ [ (2S) -2- [ [2- [ [2- [ [ (2S) -2-amino-3-phenylpropanoyl] amino] acetyl] amino] acetyl] amino] -3-phenylpropanoyl] amino] -3-hydroxybutanoyl] amino] acetyl] amino] propanoic acid. CAS No. 178249-42-8. Molecular formula: C31H41N7O9. Mole weight: 655.7.
Nociceptin (1-7) acetate
Nociceptin (1-7) acetate is a potent opioid receptor-like 1 (ORL1) receptor agonist, which in combination with nociceptin can reduce hyperalgesia and has antinociceptive activity. Synonyms: L-Alanine, N-[N-[N-[N-[N-(N-L-phenylalanylglycyl)glycyl]-L-phenylalanyl]-L-threonyl]glycyl]-, acetate; L-Phenylalanylglycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanine acetate; 1-7-Orphanin FQ (pig) acetate; H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-OH.CH3CO2H. Grades: ≥95%. Molecular formula: C31H41N7O9. Mole weight: 655.70.
[Arg14, Lys15]Nociceptin
[Arg14, Lys15]Nociceptin. Group: Biochemicals. Grades: Purified. CAS No. 236098-40-1. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
[Arg14,Lys15]Nociceptin
[Arg14,Lys15]Nociceptin behaves as a highly potent agonist of the OP(4) receptor (EC50 = 1 nM) and is able to produce long-lasting effects in vivo, compared with the natural ligand NC. It exhibits > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively). Synonyms: H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Arg-Lys-Asn-Gln-OH; [Arg(14),Lys(15)]NC. CAS No. 236098-40-1. Molecular formula: C82H137N31O22. Mole weight: 1909.18.
[Nphe1]Nociceptin(1-13)NH2
[Nphe1]Nociceptin(1-13)NH2 acts as the first truly selective and competitive nociceptin receptor antagonist and is devoid of any residual agonist activity. It binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo. Synonyms: (S, Z)-6-amino-N-((S, Z)-1-(((S, Z)-1-(((S, Z)-1-(((S)-6-amino-1-hydroxy-1-iminohexan-2-yl)imino)-5-guanidino-1-hydroxypentan-2-yl)imino)-1-hydroxypropan-2-yl)imino)-1, 3-dihydroxypropan-2-yl)-2-((Z)-((4Z, 7Z, 10Z, 12S, 13Z, 15S, 16Z, 19Z, 21S, 22Z, 24S)-12-benzyl-24-(3. CAS No. 267234-08-2. Molecular formula: C61H100N22O15. Mole weight: 1381.6.
[Nphe1]Nociceptin(1-13)NH2
[Nphe1]Nociceptin(1-13)NH2. Group: Biochemicals. Grades: Purified. CAS No. 267234-08-2. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
[(pF)Phe4]Nociceptin(1-13)NH2
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80), with 8000-fold selectivity over δ, κ, and μ opioid receptors. Synonyms: (S, Z)-6-amino-N-((S, Z)-1-(((S, Z)-1-(((S, Z)-1-(((S)-6-amino-1-hydroxy-1-iminohexan-2-yl)imino)-5-guanidino-1-hydroxypentan-2-yl)imino)-1-hydroxypropan-2-yl)imino)-1, 3-dihydroxypropan-2-yl)-2-((Z)-((2S, 3Z, 5S, 6Z, 9Z, 11S, 12Z, 14S, 15Z, 18Z, 21Z, 23S)-23-amino-2-(3-. CAS No. 380620-88-2. Molecular formula: C61H99FN22O15. Mole weight: 1399.6.
[(pF)Phe4]Nociceptin(1-13)NH2 acetate
[(pF)Phe4]Nociceptin(1-13)NH2 acetate is a highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide. It has relatively long lasting pronociceptive, hypotensive, negative inotropic and feeding stimulation effects in vivo. Grades: 98%. Molecular formula: C63H103FN22O17. Mole weight: 1459.63.
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is the first selective antagonist to prevent the binding of the endogenous ligand orphanin FQ?/Nociceptin (OFQ?/N) at the orphan opioid-like receptor, demonstrated both in vitro and in vivo. It is selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively). Synonyms: (2S) -6-amino-2- [ [ (2S) -2- [ [ (2S) -2- [ [ (2S) -2- [ [ (2S) -6-amino-2- [ [ (2S) -2- [ [ (2S) -2- [ [2- [ [ (2S, 3R) -2- [ [ (2S) -2- [ [2- [ [2- [ [ (2S) -2-amino-3-phenylpropyl] amino] acetyl] amino] acetyl] amino] -3-phenylpropanoyl] amino] -3-hydroxybutanoyl] amino] acetyl] amino] propanoyl] amino] -5- (diaminomethylideneamino) pentanoyl] amino] hexanoyl] amino] -3-hydroxypropanoyl] amino] propanoyl] amino] -5- (diaminomethylideneamino) pentanoyl] amino] hexanamide; N-[(2S)-2-Amino-3-phenylpropyl]glycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysinamide; N-[(2S)-2-Amino-3-phenylpropyl]-13-L-lysinamide-2-13-orphanin FQ (swine). CAS No. 213130-17-7. Molecular formula: C61H102N22O14. Mole weight: 1367.6.
Ac-RYYRIK-NH2 acetate
Ac-RYYRIK-NH2 acetate is a potent and partial agonist on ORL1 transfected in CHO cells (Kd = 1.5 nM). Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain. Synonyms: Ac-Arg-Tyr-Tyr-Arg-Ile-Lys-NH2.CH3CO2H; N-acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-isoleucyl-L-lysinamide acetic acid. Grades: ≥95%. CAS No. 2863659-08-7. Molecular formula: C46H74N14O11. Mole weight: 999.17.
Ac-RYYRWK-NH2 acetate
Ac-RYYRWK-NH2 acetate is a potent and selective partial agonist of the nociceptin receptor (NOP), which is the endogenous ORL1 receptor agonist. Synonyms: Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH2.CH3CO2H; N-acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-tryptophyl-L-lysinamide acetic acid. Grades: ≥95%. CAS No. 2863657-54-7. Molecular formula: C51H73N15O11. Mole weight: 1072.22.
Ac-RYYRWK-NH2 TFA
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP). Synonyms: Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH2.TFA; N-acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-tryptophyl-L-lysinamide trifluoroacetic acid; L-Lysinamide, N2-acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-tryptophyl-, mono(trifluoroacetate) (salt). Grades: ≥95%. CAS No. 408305-09-9. Molecular formula: C51H70F3N15O11. Mole weight: 1126.19.
AT-121
T-121 is a dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively). AT-121 can decrease capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner. Synonyms: AT-121; 2099681-31-7; N-[2-[1,2-dihydro-1'-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4'-piperidin]-2-yl]ethyl]-sulfamide; 3-oxo-1'-(4-propan-2-ylcyclohexyl)-2-[2-(sulfamoylamino)ethyl]spiro[1H-isoquinoline-4,4'-piperidine]; SCHEMBL18920959; SCHEMBL20230173; SCHEMBL21179793; DTXSID801336428; GLXC-25688; EX-A8003; AKOS040755934; HY-112692; CS-0062666; Q56448036; N-{2-[1'-(cis-4-Isopropylcyclohexyl)-3-oxo-1H-spiro[isoquinoline-4,4'-piperidin]-2(3H)-yl]ethyl}sulfuric diamide. Grades: ≥95%. CAS No. 2099681-31-7. Molecular formula: C24H38N4O3S. Mole weight: 462.65.
(±)-J 113397
(+/-)-J 113397 has been found to be a NOP receptor antagonist and could restrain nociceptin/orphanin FQ-induced hyperalgesia in the mouse tail-flick test. Synonyms: (±)-J 113397; (±)-J113397; (±)-J-113397; (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one. Grades: ≥98% by HPLC. CAS No. 217461-40-0. Molecular formula: C24H37N3O2. Mole weight: 399.57.
(±)-J-113397
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a K i of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC 50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 217461-40-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-107721.
MCOPPB
MCOPPB is a drug which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07 and much weaker activity at other opioid receptors. MCOPPB exhibited potent anxiolytic effects in mouse models, and inhibited signaling through nociceptin receptor in the mouse brain. Synonyms: 1-[1-(1-methylcyclooctyl)piperidin-4-yl]-2-[(3R)-piperidin-3-yl]benzimidazole. Grades: >98%. CAS No. 1028969-49-4. Molecular formula: C26H40N4. Mole weight: 408.634.
MCOPPB triHydrochloride
The trihydrochloride salt form of MCOPPB, an effective full agonist of nociceptin receptor, could be a good antianxiety agent with few side-effects. pKi: 10.07. Uses: The trihydrochloride salt form of mcoppb could be a good antianxiety agent with few side-effects. Synonyms: 1-[1-(1-methylcyclooctyl)piperidin-4-yl]-2-[(3R)-piperidin-3-yl]benzimidazole; trihydrochloride; MCOPPBtrihydrochloride; 1028969-49-4; 1108147-88-1; 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-(3R)-3-piperidinyl-1H-Benzimidazoletrihydrochloride. Grades: 95%. CAS No. 1108147-88-1. Molecular formula: C26H40N4.3HCL. Mole weight: 518.01.
MCOPPB Trihydrochloride
A potent non-peptide nociceptin/orphanin FQ peptide (NOP)-receptor full agonist [or opioid-receptor-like-1 (ORL1) receptor agonist]. It is the most potent, non-peptide NOP full agonists in vitro and a potent anxiolytic in the mice. It inhibited signaling through the NOP receptor in the mouse brain, suggesting that it penetrated into the brain after it was orally administered. It did not affect locomotor activity or memory, nor did it contribute to ethanol-induced hypnosis. Group: Biochemicals. Alternative Names: 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-(3R)-3-piperidinyl-1H-benzimidazole TriHydrochloride; PF-01678059. Grades: Highly Purified. CAS No. 1108147-88-1. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
NNC 63-0532
NNC 63-0532 is a non-peptide agonist for the nociceptin (NOP) receptor (Ki = 7.3 nM, EC50 = 305 nM). Synonyms: 1,3,8-Triazaspiro[4.5]decane-3-acetic acid, 8-(1-naphthalenylmethyl)-4-oxo-1-phenyl-, methyl ester; NNC 63 0532; NNC630532; NNC-63-0532; NNC-630532; 8-(1-Naphthalenylmethyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decane-3-acetic acid, methyl ester; Methyl 8-(1-naphthalenylmethyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decane-3-acetate. Grades: ≥98% by HPLC. CAS No. 250685-44-0. Molecular formula: C27H29N3O3. Mole weight: 443.54.
NocII
NocII, a heptadecapeptide whose sequence lies immediately downstream of nociceptin, stimulates locomotion in mice, possibly through a novel specific receptor. Synonyms: NocII; 188119-47-3; Orphanin FQ 2 (mouse); AKOS024456395; PD079090. CAS No. 188119-47-3. Molecular formula: C92H141N23O28S2. Mole weight: 2081.4.
Nocistatin (bovine)
Nocistatin (bovine) is a peptide derived from the same precursor as nociceptin, and acts as a negative control of nociceptin. It blocks nociceptin-induced allodynia and hyperalgesia, and attenuates pain evoked by prostaglandin E2. Synonyms: Nocistatin (bovine); 208253-85-4; AKOS024456394; NCGC00167175-01; PD079088. CAS No. 208253-85-4. Molecular formula: C82H135N21O32. Mole weight: 1927.07.
Orphanin FQ (1-11)
Orphanin FQ is a NOP agonist and it shows analgesic properties. Synonyms: H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-OH; L-phenylalanyl-glycyl-glycyl-L-phenylalanyl-L-threonyl-glycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanine; 1-11-Orphanin FQ (pig); 1-11-Orphanin FQ (swine); Nociceptin (1-11). Grades: ≥98% by HPLC. CAS No. 178249-41-7. Molecular formula: C49H75N15O14. Mole weight: 1098.20.
Orphanin FQ (1-11) acetate
Orphanin FQ (1-11) acetate, the peptide fragment containing amino acids 1-11 of Nociceptin, is a potent agonist of the ORL1/KOR-3 receptor with a Ki of 55 nM. Orphanin FQ is a NOP agonist with analgesic effects. Synonyms: H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-OH.CH3CO2H; L-phenylalanyl-glycyl-glycyl-L-phenylalanyl-L-threonyl-glycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanine acetate; 1-11-Orphanin FQ (pig) acetate; 1-11-Orphanin FQ (swine) acetate. Grades: ≥95%. Molecular formula: C51H79N15O16. Mole weight: 1158.26.
SB 612111
SB 612111 hydrochloride is a selective nociceptin/orphanin FQ (NOP) receptor antagonist (Ki value 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively). It modulates the pronociceptive action of nociceptin in an acute pain model and enhances morphine action in morphine-tolerant animals and inhibits hyperalgesia in an inflammatory pain model. Synonyms: SB 612111 hydrochloride; SB612111 hydrochloride; SB-612111 hydrochloride; (5S,7S)-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol hydrochloride. Grades: 99%. CAS No. 371980-98-2. Molecular formula: C24H29Cl2NO. Mole weight: 418.4.
SB 612111 hydrochloride
SB 612111 hydrochloride is a selective NOP receptor antagonist (Ki = 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors, respectively). SB 612111 exhibits antagonist activity at the pronociceptive action of nociceptin in an acute pain model. SB 612111 potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model. Synonyms: SB 612111 hydrochloride; SB612111 hydrochloride; SB-612111 hydrochloride; 7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride. Grades: ≥97% by HPLC. CAS No. 371980-94-8. Molecular formula: C24H29Cl2NO.HCl. Mole weight: 454.86.
SCH 221510
SCH 221510 is a potent and selective nociceptin opioid receptor (NOP) agonist (EC50 = 12, 693, 683 and 8071 nM, and Ki = 0.3, 65, 131 and 2854 nM at NOP, μ-, κ- and δ-opioid receptors, respectively). SCH 221510 exhibits anxiolytic-like activity at doses that have no effect on overt behaviors such as locomotion in vivo. SCH 221510 is used as the therapy of neuropathic and inflammatory pain. Uses: Potential anti-inflammatory agent. Synonyms: SCH221510; SCH 221510; SCH-221510; 3-Endo-8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol. Grades: ≥99% by HPLC. CAS No. 322473-89-2. Molecular formula: C28H31NO. Mole weight: 397.55.
SCH 221510
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC 50 of 12 nM and K i of 0.3 nM. SCH 221510 shows an anxiolytic-like effect [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 322473-89-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-107722.
Trap 101
Trap 101 is a potent and selective nociceptin/orphanin FQ (NOP) receptor antagonist (pA2 = 7.75) with selectivity for NOP receptors over classical opioid receptors (pKi = 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively). Trap 101 attenuates motor deficits in a rat model of Parkinson's Disease. Synonyms: 2H-Benzimidazol-2-one, 1-[1-(cyclooctylmethyl)-1,2,3,6-tetrahydro-5-(hydroxymethyl)-4-pyridinyl]-3-ethyl-1,3-dihydro-; 1-[1-(Cyclooctylmethyl)-1,2,3,6-tetrahydro-5-(hydroxymethyl)-4-pyridinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one; Trap-101; Trap101; 1-[1-(cyclooctylmethyl)-5-(hydroxymethyl)-3,6-dihydro-2H-pyridin-4-yl]-3-ethyl-2-benzimidazolone. Grades: ≥95%. CAS No. 873567-76-1. Molecular formula: C24H35N3O2. Mole weight: 397.55.
UFP-101
UFP-101 is a potent, selective and competitive silent antagonist for the NOP opioid receptor, displaying > 3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 exhibits antinociceptive activity by opposing the action of nociceptin in vivo. Synonyms: UFP-101; UFP 101; UFP101. Grades: >98%. CAS No. 849024-68-6. Molecular formula: C82H138N32O21. Mole weight: 1908.19.
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