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MedKoo Cat#: 526248 | Name: SAR114137-analog

Description:

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

SAR114137-Analog was previously mistakenly listed as SAR114137. SAR114137-analog has CAS#537706-31-3. The correct structure was published in Eur J Pharm Biopharm. 2013 Apr;83(3):436-48. SAR114137 has CAS#958853-11-7. SAR-114137 is a novel, orally available inhibitor of cysteine cathepsin. It is developed for the use in chronic pain. SAR114137-analog structure is completely different than SAR114137.

Chemical Structure

SAR114137-analog
SAR114137-analog
CAS#537706-31-3

Theoretical Analysis

MedKoo Cat#: 526248

Name: SAR114137-analog

CAS#: 537706-31-3

Chemical Formula: C25H34N4O7S

Exact Mass: 534.2148

Molecular Weight: 534.63

Elemental Analysis: C, 56.17; H, 6.41; N, 10.48; O, 20.95; S, 6.00

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 #
958853-11-7 537706-31-3
Synonym
SAR114137-analog; SAR 114137-analog; SAR 114137-analog
IUPAC/Chemical Name
4-Morpholinebutanamide, alpha-(((2-methylpropyl)sulfonyl)methyl)-gamma-oxo-N-((1S)-1-((5-phenyl-1,2,4-oxadiazol-3-yl)carbonyl)propyl)-
InChi Key
IUMMRYVGHFJSRD-ANYOKISRSA-N
InChi Code
InChI=1S/C25H34N4O7S/c1-4-20(22(31)23-27-25(36-28-23)18-8-6-5-7-9-18)26-24(32)19(16-37(33,34)15-17(2)3)14-21(30)29-10-12-35-13-11-29/h5-9,17,19-20H,4,10-16H2,1-3H3,(H,26,32)/t19?,20-/m0/s1
SMILES Code
O=C(N[C@H](C(C1=NOC(C2=CC=CC=C2)=N1)=O)CC)C(CS(=O)(CC(C)C)=O)CC(N3CCOCC3)=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
SAR114137 is a potent inhibitor of human cathepsin S (Ki: 6 nM) and is 3- to 4-fold less active against cathepsin K (Ki: 16 nM). Cathepsin S inhibition was confirmed in vivo as oral administration of SAR114137 to mice inhibited the cathepsin S-dependent processing of MHCII in spleen. Shows analgesic-like properties in chronic pain models induced by inflammation/cartilage degradation or by nerve injury. Robust pain lowering efficacy in range <1 μg to <1 mg/kg in mouse with efficacy seen at 1 mg/kg in all tested species. Has a rapid onset of action in pain models (1-2 h) and a long duration of action (i.e., 3 days after last admin.) but no PK/PD relationship (short half-life). It is active in a wide range from (1, 10 mg/kg) and shows no anti-inflammatory activity.

Preparing Stock Solutions

The following data is based on the product molecular weight 534.63 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.

Recalculate based on batch purity %
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: Petzoldt C, Bley O, Byard SJ, Andert D, Baumgartner B, Nagel N, Tappertzhofen C, Feth MP. An example of how to handle amorphous fractions in API during early pharmaceutical development: SAR114137--a successful approach. Eur J Pharm Biopharm. 2014 Apr;86(3):337-50. doi: 10.1016/j.ejpb.2013.09.015. PubMed PMID: 24075979. 2: Feth MP, Heyse W, Baumgartner B, Nagel N, Tappertzhofen C, Olpp T, Jurascheck J, Ulrich J, Helmdach L, Petzoldt C. From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor. Eur J Pharm Biopharm. 2013 Apr;83(3):436-48. doi: 10.1016/j.ejpb.2012.11.007. PubMed PMID: 23201054.

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