Product Information
Applications
Biological Information
Primary TargetPrCP
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

PrCP Inhibitor - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Wu, Z., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1774.
Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett. 22, 658.
Zhou, C., et al. 2010. J. Med. Chem. 53, 7251.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision11-October-2013 JSW
Synonyms2-Amino-N-((2S,3S)-3-(biphenyl-4-yl)-1-((2S)-2-(5,6-dichloro-1H-benzimidazol-2-yl)pyrrolidin-1-yl)-1-oxobutan-2-yl)-2-methylpropanamide, Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor
DescriptionA dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 in the absence/presence of 1% mouse serum albumin = 1 nM/1 nM and 2 nM/8 nM, respectively, against human and mouse PrCP-catalyzed Mca-APK(Dnp)-OH hydrolysis; Initial [Substrate] = 25 µM), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC50 >25 µM). Despite its being a substrate of P-gp efflux transporters and ineffective CNS delivery across blood-brain barrier, peripheral PrCP inhibition via oral administration (100 mg/kg/d for 5 d; [Drug] = 380 nM and 50 nM, respectively, in blood and brain 24 h after last p.o. dosing) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice (0.73 g fat reduction vs. 0,73 g fat gain in 5 d, respectively, with drug or vehicle treatment) in vivo. Drug treatment among PrCP-/- obsese mice in comparison, results in only 1.1% weight loss primarily due to a decreased gain in muscle mass and little change in body fat.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₁H₃₃Cl₂N₅O₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage -20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesWu, Z., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1774.
Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett. 22, 658.
Zhou, C., et al. 2010. J. Med. Chem. 53, 7251.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Proteases Inhibitors