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Upacicalcet

Cat. No. M21421
Upacicalcet Structure
Size Price Availability Quantity
5mg USD 480  USD480 In stock
10mg USD 650  USD650 In stock
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Biological Activity

Upacicalcet is a calcium-sensing receptor (CaSR) agonist being developed for the study of secondary hyperparathyroidism (SHPT).

Chemical Information
Molecular Weight 351.76
Formula C11H14ClN3O6S
CAS Number 1333218-50-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hirofumi Sato, et al. Bone. Upacicalcet, a positive allosteric modulator of the calcium-sensing receptor, prevents vascular calcification and bone disorder in a rat adenine-induced secondary hyperparathyroidism model

[2] Hirofumi Sato, et al. Mol Pharmacol. Upacicalcet Is a Novel Secondary Hyperparathyroidism Drug that Targets the Amino Acid Binding Site of Calcium-Sensing Receptor

[3] Junichiro James Kazama, et al. Clin Pharmacokinet. First-in-Patient Phase I/II Study of Upacicalcet in Japanese Patients with Secondary Hyperparathyroidism Undergoing Hemodialysis: Pharmacokinetic and Pharmacodynamic Properties

[4] Fumihiko Koiwa, et al. Drugs R D. First-in-Human Phase I Study of the Novel Injectable Calcimimetic Agent Upacicalcet in Healthy Adult Japanese Participants

[5] Sheridan M Hoy. Drugs. Upacicalcet: First Approval

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Keywords: Upacicalcet supplier, Calcium-sensing Receptor, inhibitors, activators

 
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