A 81988

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

MedKoo CAT#: 571215

CAS#: 141887-34-5

Description: A 81988 is a selective angiotensin II antagonist for type I receptors. It is a potent, competitive, non-peptidic antagonist of angiotensin AT1 receptors.


Price and Availability

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A 81988 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#: 571215
Name: A 81988
CAS#: 141887-34-5
Chemical Formula: C23H22N6O2
Exact Mass: 414.1804
Molecular Weight: 414.47
Elemental Analysis: C, 66.65; H, 5.35; N, 20.28; O, 7.72


Synonym: A 81988; A-81988; A81988; Abbott 81988; Abbott-81988

IUPAC/Chemical Name: 3-Pyridinecarboxylic acid, 2-(propyl((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)amino)-

InChi Key: DLMNZGAILMQDHA-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H22N6O2/c1-2-14-29(22-20(23(30)31)8-5-13-24-22)15-16-9-11-17(12-10-16)18-6-3-4-7-19(18)21-25-27-28-26-21/h3-13H,2,14-15H2,1H3,(H,30,31)(H,25,26,27,28)

SMILES Code: O=C(C1=CC=CN=C1N(CCC)CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)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

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: Lee JY, Warner RB, Brune ME, Adler AL, Winn M, De B, Zydowsky TM, Opgenorth TJ, Kerkman DJ, DeBernardis JF. Cardiovascular effects of orally administered ABBOTT-81988, an angiotensin II antagonist, in conscious spontaneously hypertensive rats. Am J Hypertens. 1994 Nov;7(11):975-83. PubMed PMID: 7848624.

2: Hancock AA, Surber BW, Rotert G, Thomas S, Tasker AS, Sorensen BK, Vodenlich AD, Opgenorth TJ, Kerkman DJ, DeBernardis JF. [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54. PubMed PMID: 8206129.

3: Pollock DM, Polakowski JS, Divish BJ, Opgenorth TJ. Angiotensin blockade reverses hypertension during long-term nitric oxide synthase inhibition. Hypertension. 1993 May;21(5):660-6. PubMed PMID: 7684026.

4: Hancock AA, Buckner SA, Lee JY, Brune M, Morse PA, Oheim K, Warner RB, Winn M, Zydowsky TM, De B, et al. Receptor interactions of Abbott-81988, a highly potent, non-peptide angiotensin-II antagonist selective for type-1 receptors. J Recept Res. 1994 May;14(3-4):229-49. PubMed PMID: 8083867.

5: Lee JY, Buckner SA, Brune ME, Warner RB, Winn M, De B, Zydowsky TM, Opgenorth TJ, Kerkman DJ, Debernardis JF. Characterization of antihypertensive activity of ABBOTT-81988, a nonpeptide angiotensin II antagonist in the renal hypertensive rat. J Pharmacol Exp Ther. 1994 Jan;268(1):427-33. PubMed PMID: 8301584.

6: Solhaug MJ, Wallace MR, Granger JP. Nitric oxide and angiotensin II regulation of renal hemodynamics in the developing piglet. Pediatr Res. 1996 Mar;39(3):527-33. PubMed PMID: 8929876.

7: Madeddu P, Anania V, Varoni MV, Parpaglia PP, Demontis MP, Fattaccio MC, Palomba D, Pollock D, Glorioso N. Prevention by blockade of angiotensin subtype1-receptors of the development of genetic hypertension but not its heritability. Br J Pharmacol. 1995 Jun;115(4):557-62. PubMed PMID: 7582472; PubMed Central PMCID: PMC1908501.

8: Madeddu P, Salis MB, Emanueli C. Altered baroreflex control of heart rate in bradykinin B2-receptor knockout mice. Immunopharmacology. 1999 Dec;45(1-3):21-7. PubMed PMID: 10614985.

9: Winn M, De B, Zydowsky TM, Altenbach RJ, Basha FZ, Boyd SA, Brune ME, Buckner SA, Crowell D, Drizin I, et al. 2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists. J Med Chem. 1993 Sep 3;36(18):2676-88. PubMed PMID: 8410980.

10: Madeddu P, Emanueli C, Maestri R, Salis MB, Minasi A, Capogrossi MC, Olivetti G. Angiotensin II type 1 receptor blockade prevents cardiac remodeling in bradykinin B(2) receptor knockout mice. Hypertension. 2000 Jan;35(1 Pt 2):391-6. PubMed PMID: 10642330.

11: Madeddu P, Varoni MV, Palomba D, Emanueli C, Demontis MP, Glorioso N, Dessì-Fulgheri P, Sarzani R, Anania V. Cardiovascular phenotype of a mouse strain with disruption of bradykinin B2-receptor gene. Circulation. 1997 Nov 18;96(10):3570-8. PubMed PMID: 9396457.

12: Madeddu P, Glorioso N. Does blockade of the renin-angiotensin system prevent heritability of genetic hypertension? Hypertension. 1995 Aug;26(2):9375. PubMed PMID: 7635550.

13: Pollock DM, Divish BJ, Polakowski JS, Opgenorth TJ. Angiotensin II receptor blockade improves renal function in rats with reduced renal mass. J Pharmacol Exp Ther. 1993 Nov;267(2):657-63. PubMed PMID: 8246138.