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505876 RXFP1 Agonist - Calbiochem

RXFP1 Agonist - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Leucine-Rich Repeat-Containing GPCR 7 Agonist, LGR7 Agonist, Relaxin/Insulin-like Family Peptide Receptor 1 Agonist, 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide

Primary Target: hRXFP1
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₁F₃N₂O₅S

Products

Catalog NumberPackaging Qty/Pack
5.05876.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable 2-acetamido-N-phenylbenzamide that selectively activates human, but not mouse, LGR7/RXFP1-mediated cAMP induction (EC50 = 200 nM in THP1) via allosteric interaction with the ECL3 region without competing against ECL2-mediated relaxin binding or affecting AVPR1B- or LGR8/RXFP2-mediated cAMP induction. Although shown to be ~150-fold and 500-fold less potent than relaxin (RLX), respectively, in VEGF mRNA induction and cellular impedance assays, pharmacokinetic studies reveal superior in vivo stability to RLX and in vivo bioavailability in mice via oral (Cmax/Tmax = 604 nM/plasma/1 h and 1026 ng/g heart/1.5 h; 30 mg/kg) or intraperitoneal (Cmax/Tmax = 9.29 µM/plasma/1 h and 28.6 µmol/kg heart/1 h; 30 mg/kg) administration with good aqueous solubility (7 µM in PBS).
Catalogue Number505876
Brand Family Calbiochem®
SynonymsLeucine-Rich Repeat-Containing GPCR 7 Agonist, LGR7 Agonist, Relaxin/Insulin-like Family Peptide Receptor 1 Agonist, 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide
References
ReferencesXiao, J., et al. 2013. Nat. Commun. 4, 1953.
Product Information
FormWhite powder
Hill FormulaC₂₄H₂₁F₃N₂O₅S
Chemical formulaC₂₄H₂₁F₃N₂O₅S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargethRXFP1
Purity≥98% 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 +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Identification Number
Catalog Number GTIN
5.05876.00014055977263121

Documentation

RXFP1 Agonist - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Xiao, J., et al. 2013. Nat. Commun. 4, 1953.
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.

Revision14-January-2014 JSW
SynonymsLeucine-Rich Repeat-Containing GPCR 7 Agonist, LGR7 Agonist, Relaxin/Insulin-like Family Peptide Receptor 1 Agonist, 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide
DescriptionA cell-permeable 2-acetamido-N-phenylbenzamide that selectively activates human, but not mouse, LGR7/RXFP1 (EC50 = 94 and 200 nM, respectively, in cAMP induction using HEK293-hRXFP1 transfectant and THP1) via allosteric interaction with the ECL3 (TM helix 5 to EC loop3; V646 to T660) region without competing against ECL2-mediated relaxin binding, while exhibiting cytotoxicity only at much higher concentrations (IC50 in 72 h = 9.4 µM in HEK293-RXFP1 cultures) and displaying no activity toward AVPR1B- (Arginine vasopressin receptor 1B) or LGR8/RXFP2-mediated cAMP induction. Although shown to be ~150-fold and 500-fold less potent than relaxin (RLX), respectively, in VEGF mRNA induction (275% of basal level in THP1 cells; 250 nM) and cellular impedance assays (in HEK293-RXFP1 cultures), pharmacokinetic studies reveal superior in vivo stability (T1/2 = 8.56 and 7.48 h in plasma and heart post single 30 mg/kg i.p. dosage in mice) to RLX (initial T1/2 <10 min in human; i.v.) and, while RLX is not orally active, this chemical agonist is demonstrated to be bioavailable in mice via oral (Cmax/Tmax = 604 nM/1 h and 1026 ng/g/1.5 h in plasma and heart, respectively; 30 mg/kg) or intraperitoneal (Cmax/Tmax = 9.29 µM/1 h and 28.6 µmol/kg/1 h in plasma and heart, respectively; 30 mg/kg) administration in vivo with good aqueous solubility (7 µM in PBS).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₄H₂₁F₃N₂O₅S
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesXiao, J., et al. 2013. Nat. Commun. 4, 1953.