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505876 RXFP1 Agonist - Calbiochem

505876
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₁F₃N₂O₅S

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      Glass bottle 10 mg
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      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

      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 +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesXiao, J., et al. 2013. Nat. Commun. 4, 1953.