A-192621

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526692

CAS#: 195529-54-5

Description: A-192621 is an endothelin-B antagonist. A-192621 markedly enhanced MAP, TPR, and mesenteric, and the renal constrictor effects of ET-1. A-192621 was more effective than IRL-2500 in blocking IRL-1620-induced vasoconstriction, but both augmented constrictor responses to ET-1.


Price and Availability

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A-192621 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526692
Name: A-192621
CAS#: 195529-54-5
Chemical Formula: C33H38N2O6
Exact Mass: 558.273
Molecular Weight: 558.675
Elemental Analysis: C, 70.95; H, 6.86; N, 5.01; O, 17.18


Synonym: A-192621; A 192621; A192621; A-192621-1; A-192621.1.

IUPAC/Chemical Name: (2R,3R,4S)-4-(benzo[d][1,3]dioxol-5-yl)-1-(2-((2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid

InChi Key: LQEHCKYYIXQEBM-FUKIBTTHSA-N

InChi Code: InChI=1S/C33H38N2O6/c1-4-16-39-25-13-10-23(11-14-25)32-30(33(37)38)26(24-12-15-27-28(17-24)41-20-40-27)18-35(32)19-29(36)34-31-21(5-2)8-7-9-22(31)6-3/h7-15,17,26,30,32H,4-6,16,18-20H2,1-3H3,(H,34,36)(H,37,38)/t26-,30-,32+/m1/s1

SMILES Code: O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Wessale JL, Adler AL, Novosad EI, Calzadilla SV, Dayton BD, Marsh KC, Winn M,
Jae HS, von Geldern TW, Opgenorth TJ, Wu-Wong JR. Pharmacology of endothelin
receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo
studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. PubMed PMID: 12193067.

2: Wu-Wong JR, Dixon DB, Chiou WJ, Sorensen BK, Liu G, Jae HS, Tasker A, von
Geldern TW, Winn M, Opgenorth TJ. Pharmacology of endothelin receptor antagonists
ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002
Aug;103 Suppl 48:107S-111S. PubMed PMID: 12193066.

3: Leung SW, Lim SL, Pang CC, Man RY. Use of A-192621 and IRL-2500 to unmask the
mesenteric and renal vasodilator role of endothelin ET(B) receptors. J Cardiovasc
Pharmacol. 2002 Apr;39(4):533-43. PubMed PMID: 11904527.

4: Cullen JP, Bell D, Kelso EJ, McDermott BJ. Use of A-192621 to provide evidence
for involvement of endothelin ET(B)-receptors in endothelin-1-mediated
cardiomyocyte hypertrophy. Eur J Pharmacol. 2001 Apr 13;417(3):157-68. PubMed
PMID: 11334846.

5: Brodsky S, Abassi Z, Wessale J, Ramadan R, Winaver J, Hoffman A. Effects of
A-192621.1, a specific endothelin-B antagonist, on intrarenal hemodynamic
responses to endothelin-1. J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S311-3.
PubMed PMID: 11078406.