Fasidotril

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

MedKoo CAT#: 326893

CAS#: 135038-57-2

Description: Fasidotril, also known as BP-1.137; BP-1137, is a NEP/ACE inhibitor potentially for the treatment of myocardial infarction (MI), hypertension and heart. Fasidotril was an effective oral antihypertensive agent during chronic treatment in high-renin renovascular rats, normal-renin SHR, and low-renin DOCA-salt hypertensive rats and in patients with essential hypertension.


Price and Availability

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Fasidotril is not in stock, but 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#: 326893
Name: Fasidotril
CAS#: 135038-57-2
Chemical Formula: C23H25NO6S
Exact Mass: 443.1403
Molecular Weight: 443.514
Elemental Analysis: C, 62.29; H, 5.68; N, 3.16; O, 21.64; S, 7.23


Synonym: BP-1.137; BP 1.137; BP1.137; BP-1137; BP 1137; BP1137; Fasidotril

IUPAC/Chemical Name: benzyl ((S)-3-(acetylthio)-2-(benzo[d][1,3]dioxol-5-ylmethyl)propanoyl)-L-alaninate

InChi Key: KKBIUAUSZKGNOA-HNAYVOBHSA-N

InChi Code: InChI=1S/C23H25NO6S/c1-15(23(27)28-12-17-6-4-3-5-7-17)24-22(26)19(13-31-16(2)25)10-18-8-9-20-21(11-18)30-14-29-20/h3-9,11,15,19H,10,12-14H2,1-2H3,(H,24,26)/t15-,19+/m0/s1

SMILES Code: C[C@@H](C(OCC1=CC=CC=C1)=O)NC([C@H](CC2=CC=C(OCO3)C3=C2)CSC(C)=O)=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: Inoue M, Sasaki T, Takazawa H, Morita T, Narisawa A, Saito A, Midorikawa H, Nishijima M. Symptomatic vasospasm in elderly patients with aneurysmal subarachnoid hemorrhage: comparison with nonelderly patients. Acta Neurochir Suppl. 2013;115:281-4. doi: 10.1007/978-3-7091-1192-5_50. PubMed PMID: 22890682.

2: Ozdener F, Ozdemir V. Fasidotril Eli Lilly. Curr Opin Investig Drugs. 2003 Sep;4(9):1113-9. Review. PubMed PMID: 14582457.

3: Monteil T, Danvy D, Sihel M, Leroux R, Plaquevent JC. Strategies for access to enantiomerically pure ecadotril, dexecadotril and fasidotril: a review. Mini Rev Med Chem. 2002 Jun;2(3):209-17. Review. PubMed PMID: 12370063.

4: Sagnella GA. Vasopeptidase inhibitors. J Renin Angiotensin Aldosterone Syst. 2002 Jun;3(2):90-5. Review. PubMed PMID: 12228848.

5: Laurent S, Boutouyrie P, Azizi M, Marie C, Gros C, Schwartz JC, Lecomte JM, Bralet J. Antihypertensive effects of fasidotril, a dual inhibitor of neprilysin and angiotensin-converting enzyme, in rats and humans. Hypertension. 2000 May;35(5):1148-53. PubMed PMID: 10818079.

6: Fasidotril. Aladotril, alatriopril, BP 1137. Drugs R D. 1999 Apr;1(4):346-7. PubMed PMID: 10566060.

7: Marie C, Mossiat C, Gros C, Schwartz JC, Lecomte JM, Bralet J. Effect of long-term therapy with fasidotril, a mixed inhibitor of neprilysin and angiotensin-converting enzyme (ACE), on survival of rats after myocardial infarction. Cardiovasc Res. 1999 Mar;41(3):544-53. PubMed PMID: 10435026.

8: Hu K, Ertl G. Potential role of mixed ACE and neutral endopeptidase inhibitor in the treatment of heart failure. Cardiovasc Res. 1999 Mar;41(3):503-5. PubMed PMID: 10435019.

9: Marie C, Mossiat C, Lecomte JM, Schwartz JC, Bralet J. Hemodynamic effects of acute and chronic treatment with aladotril, a mixed inhibitor of neutral endopeptidase and angiotensin I-converting enzyme, in conscious rats with myocardial infarction. J Pharmacol Exp Ther. 1995 Dec;275(3):1324-31. PubMed PMID: 8531099.