CaSR agonist peptide-1
CaSR agonist peptide-1 is a human calcium-sensing receptor (CaSR) agonist. CaSR agonist peptide-1 activates CaSR by binding to it. CaSR agonist peptide-1 can be used in studies related to secondary hyperparathyroidism.
For research use only. We do not sell to patients.
- CAS No.: 3057162-39-4
- Formula: C43H75N21O10S2
- Molecular Weight:1110.32
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
CaSR agonist peptide-1 (compound 6g) (60 min) acts as a positive allosteric modulator of human CaSR in Flp-In-HEK293-CASR cells, with an EC50 of 2.89 μM in the presence of 1.2 mM Ca2+[1].
CaSR agonist peptide-1 does not inhibit human CYP1A2, 2C9, 2C19, 2D6, or 3A4 at concentrations up to 50 μM in human liver microsomes[1].
CaSR agonist peptide-1 shows moderate metabolic stability in human and rat liver microsomes, with ~35% remaining after 60 min of incubation at 5 μM[1].
CaSR agonist peptide-1 exhibits desirable plasma stability across mouse, rat, dog, monkey, and human plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CaSR agonist peptide-1 (1 mg/kg; i.v.; single dose) produces sustained, significant suppression of plasma PTH (persisting 24 h), reduced serum Ca2+, and biphasic modulation of serum P in male Sprague-Dawley rats with 5/6 nephrectomy-induced SHPT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male, 200-220 g)[1]
-
Dosage:0.3 mg/kg
-
Administration:i.v.; single dose
-
Result:Significantly reduced plasma PTH levels versus the Etelcalcetide group at 1 h postdose.
Demonstrated greater PTH-lowering efficacy than Etelcalcetide at the equivalent dose.
-
Animal Model:Sprague-Dawley (male, 5/6 nephrectomy + 4 weeks high-phosphorus diet)[1]
-
Dosage:1 mg/kg
-
Administration:i.v.; single dose
-
Result:Reduced plasma PTH markedly at 1 and 6 h, effects sustained 24 h.
Lowered serum Ca significantly at 1 h, effects maintained 48 h.
Elicited biphasic serum P: decreased at 1 h, increased at 6 h.
Chemical Information
-
CAS No. 3057162-39-4
-
Molecular Weight 1110.32
-
Formula C43H75N21O10S2
-
Sequence
Ac-{d-Cys(L-Cys)}-{d-Arg}-{d-Phe(3-Gu)}-{d-Abu}-{d-Arg}-{d-Ala}-{d-Arg}-NH2
-
Sequence Shortening
Ac-{d-Cys(L-Cys)}-{d-Arg}-{d-Phe(3-Gu)}-{d-Abu}-{d-Arg}-{d-Ala}-{d-Arg}-NH2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CaSR agonist peptide-1 Related Classifications
HY-P11832 Related Classifications
Powered by Bioz