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Choose fixed kits that allow you to explore entire pathways or processes. Or design your own kits by choosing single plex MAPmates™, following the provided guidelines.
The following MAPmates™ should not be plexed together:
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Buffer Detection Kit for Magnetic Beads
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504044
Sigma-AldrichPrCP Inhibitor - CAS 1252037-41-4 - Calbiochem
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Description
Overview
A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 = 1 nM against human PrCP; IC50 = 2 and 8 nM against mouse PrCP, respectively, in the absence or presence of 1% mouse serum albumin), 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). Oral administration (100 mg/kg/d for 5 d) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice in vivo.
Catalogue Number
504044
Brand Family
Calbiochem®
Synonyms
Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-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
References
References
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.
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.
Revision
11-October-2013 JSW
Synonyms
Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-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
Description
A 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.
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1252037-41-4
Chemical formula
C₃₁H₃₃Cl₂N₅O₂
Structure formula
Purity
≥97% by HPLC
Solubility
DMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.