2. GPCR/G Protein
  3. RXFP Receptor
  4. RXFP1 receptor agonist-9

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 of 2.5 μM and Ymax of 65%. RXFP1 receptor agonist-9 exhibits good microsomal stability, reasonable PK and pharmacological activity. RXFP1 receptor agonist-9 can be used to the study of heart failure.

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RXFP1 receptor agonist-9 Chemical Structure

RXFP1 receptor agonist-9 Chemical Structure

CAS No. : 2924765-23-9

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RXFP1 receptor agonist-9 Related Antibodies

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Description

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 of 2.5 μM and Ymax of 65%. RXFP1 receptor agonist-9 exhibits good microsomal stability, reasonable PK and pharmacological activity. RXFP1 receptor agonist-9 can be used to the study of heart failure[1].

Parmacokinetics[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 4.43 hr
Rat 10 mg/kg p.o. F 6 %
Rat 1 mg/kg i.v. AUC 9.6 μM·h
Rat 1 mg/kg i.v. Vss 0.09 L/kg
Rat 1 mg/kg i.v. CL 2.5 mL/min/kg
In Vivo

RXFP1 receptor agonist-9 (Compound 39) (0.5, 1.5, 5 mg/min/kg, i.v., daily for 21 days) induces a dose-dependent heart rate increase (consistent with the hemodynamic profile of relaxin) in isoflurane-anesthetized naïve rats[1].
RXFP1 receptor agonist-9 (25 mg/kg, i.v., respectively on day 6 and 7) elicites significant interpubic ligament (IPL) expansion, which recapitulated the effect of relaxin in C57BL/6 mouse[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Isoflurane-anesthetized male Sprague Dawley (SD) rat model
Dosage: 5 mg/min/kg
Administration: IV, 60 min
Result: Induced a 25% increase on heart rate.
Animal Model: Isoflurane-anesthetized male Sprague Dawley (SD) rat model
Dosage: 0.5 mg/min/kg, 1.5 mg/min/kg, 5 mg/min/kg,
Administration: IV, 60 min
Result: Observed a dose-dependent increase at 1.5 and 5 mg/min/kg while no major effect was observed at 0.5 mg/min/kg.
Animal Model: Baseline microCT scan acquired for the estrogen primed C57BL/6 female mice pubis (primed with estrogen on day 0)
Dosage: 25 mg/kg,
Administration: IV, respectively on day 6 and 7
Result: Showed 500% symphysis widening, and thus IPL expansion.
Molecular Weight

727.67

Formula

C37H34F5N3O7
CAS No.
SMILES

O=C(N[C@@H]1[C@@H]2CC[C@H]([C@@H]1C(NC3=CC(C(F)(F)F)=C(C=C3)F)=O)/C2=C/C4CC4)C5=CC(C6=C(C=CC(C(C(O)=O)OC(NC)=O)=C6)F)=CC=C5OC
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RXFP1 receptor agonist-9 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

RXFP1 receptor agonist-92924765-23-9RXFP ReceptorRelaxin family peptideNorbornyl BisamidesRelaxinHuman relaxin-2Heart failureInhibitorinhibitorinhibit

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RXFP1 receptor agonist-9
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