Sampatrilat | UK-81252 | CAS#129981-36-8 | NEP/ACE inhibitor

MedKoo Cat#: 328020 | Name: Sampatrilat

Description:

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

Sampatrilat, aslo known as UK-81252, is a NEP/ACE inhibitor potentially for the treatment of hypertension and heart failure.

Chemical Structure

Sampatrilat

CAS#129981-36-8

Theoretical Analysis

MedKoo Cat#: 328020

Name: Sampatrilat

CAS#: 129981-36-8

Chemical Formula: C26H40N4O9S

Exact Mass: 584.2516

Molecular Weight: 584.69

Elemental Analysis: C, 53.41; H, 6.90; N, 9.58; O, 24.63; S, 5.48

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

Sampatrilat; UK-81252; UK 81252; UK81252; UK-81,252; UK 81,252; UK81,252.

IUPAC/Chemical Name

(S)-3-((S)-6-amino-2-(methylsulfonamido)hexanamido)-4-(1-(((S)-1-carboxy-2-(4-hydroxyphenyl)ethyl)carbamoyl)cyclopentyl)butanoic acid

InChi Key

DGTDHMSPXWLPNJ-GIVPXCGWSA-N

InChi Code

InChI=1S/C26H40N4O9S/c1-40(38,39)30-20(6-2-5-13-27)23(34)28-18(15-22(32)33)16-26(11-3-4-12-26)25(37)29-21(24(35)36)14-17-7-9-19(31)10-8-17/h7-10,18,20-21,30-31H,2-6,11-16,27H2,1H3,(H,28,34)(H,29,37)(H,32,33)(H,35,36)/t18-,20+,21+/m1/s1

SMILES Code

O=C(O)C[C@H](CC1(C(N[C@H](C(O)=O)CC2=CC=C(O)C=C2)=O)CCCC1)NC([C@H](CCCCN)NS(=O)(C)=O)=O

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).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 584.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

. 1: Machowska A, Juszczak K, Novak P, Thor P. The natriuretic peptide neurohormonal system modulation by vasopeptidase inhibitors--the novel therapeutical approach of hypertension treatment. Folia Med Cracov. 2009;50(3-4):35-42. Review. PubMed PMID: 21853869. 2: Chang RK, Shojaei AH. Effect of a lipoidic excipient on the absorption profile of compound UK 81252 in dogs after oral administration. J Pharm Pharm Sci. 2004 Jan 23;7(1):8-12. PubMed PMID: 15144729. 3: Gurzu B, Costuleanu M, Petrescu G. [Alternative pathways for the activation of the renin-angiotensin system]. Rev Med Chir Soc Med Nat Iasi. 2003 Oct-Dec;107(4):710-7. Review. Romanian. PubMed PMID: 14756007. 4: Maki T, Nasa Y, Tanonaka K, Takahashi M, Takeo S. Beneficial effects of sampatrilat, a novel vasopeptidase inhibitor, on cardiac remodeling and function of rats with chronic heart failure following left coronary artery ligation. J Pharmacol Exp Ther. 2003 Apr;305(1):97-105. PubMed PMID: 12649357. 5: Sagnella GA. Vasopeptidase inhibitors. J Renin Angiotensin Aldosterone Syst. 2002 Jun;3(2):90-5. Review. PubMed PMID: 12228848. 6: Allikmets K. Sampatrilat Shire. Curr Opin Investig Drugs. 2002 Apr;3(4):578-81. PubMed PMID: 12090727. 7: Nathisuwan S, Talbert RL. A review of vasopeptidase inhibitors: a new modality in the treatment of hypertension and chronic heart failure. Pharmacotherapy. 2002 Jan;22(1):27-42. Review. PubMed PMID: 11794428. 8: Asher JR, Naftilan AJ. Vasopeptidase inhibition: a new direction in cardiovascular treatment. Curr Hypertens Rep. 2000 Aug;2(4):384-91. Review. PubMed PMID: 10981174. 9: Sampatrilat. UK 81252. Drugs R D. 1999 Apr;1(4):352-3. PubMed PMID: 10566063. 10: Norton GR, Woodiwiss AJ, Hartford C, Trifunovic B, Middlemost S, Lee A, Allen MJ. Sustained antihypertensive actions of a dual angiotensin-converting enzyme neutral endopeptidase inhibitor, sampatrilat, in black hypertensive subjects. Am J Hypertens. 1999 Jun;12(6):563-71. PubMed PMID: 10371365. 11: Wallis EJ, Ramsay LE, Hettiarachchi J. Combined inhibition of neutral endopeptidase and angiotensin-converting enzyme by sampatrilat in essential hypertension. Clin Pharmacol Ther. 1998 Oct;64(4):439-49. PubMed PMID: 9797801. 12: Venn RF, Barnard G, Kaye B, Macrae PV, Saunders KC. Clinical analysis of sampatrilat, a combined renal endopeptidase and angiotensin-converting enzyme inhibitor II: assay in the plasma and urine of human volunteers by dissociation enhanced lanthanide fluorescence immunoassay (DELFIA). J Pharm Biomed Anal. 1998 Jan;16(5):883-92. PubMed PMID: 9535200. 13: Venn RF, Kaye B, Macrae PV, Saunders KC. Clinical analysis of sampatrilat, a combined renal endopeptidase and angiotensin-converting enzyme inhibitor I: assay in plasma of human volunteers by atmospheric-pressure ionisation mass-spectrometry following derivatisation with BF3-methanol. J Pharm Biomed Anal. 1998 Jan;16(5):875-81. PubMed PMID: 9535199. 14: Kirk JE, Wilkins MR. Renal effects of concurrent E-24.11 and ACE inhibition in the aorto-venocaval fistula rat. Br J Pharmacol. 1996 Nov;119(5):943-8. PubMed PMID: 8922744; PubMed Central PMCID: PMC1915920.