2. GPCR/G Protein
  3. CaSR
  4. 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.

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CaSR agonist peptide-1

CaSR agonist peptide-1 Chemical Structure

CAS No. : 3057162-39-4

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CaSR agonist peptide-1 Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

CaSR agonist peptide-1 (compound 6g) (0.3 mg/kg; i.v.; single dose) produces greater single-dose PTH-lowering efficacy than Etelcalcetide (HY-P1955) in normal male Sprague-Dawley rats[1].
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.
Molecular Weight

1110.32

Formula

C43H75N21O10S2
CAS No.
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
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CaSR agonist peptide-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CaSR agonist peptide-13057162-39-4CaSR agonist peptide1CaSR agonist peptide 1CaSRCalcium-sensing receptorCYP3A4calcium-sensing receptorCYP1A2CYP2C19CYP2C9extracellular domainCYP2D6Flp-In-HEK293-CASR cellssecondary hyperparathyroidismInhibitorinhibitorinhibit

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