PCO371 is a novel, orally active small molecule full agonist of PTHR1. PCO371 does not affect the PTH type 2 receptor (PTHR2). Oral administration of PCO371 to osteopenic rats provokes a significant increase in bone turnover with limited increase in bone mass. In hypocalcemic rats, PCO371 restores serum calcium levels without increasing urinary calcium, and with stronger and longer-lasting effects than PTH injections. PCO371 induces cAMP production with an EC50 of 2.4 μM in COS-7 cells expressing hPTHR1, and 2.5 μM in COS-7 cells transfected with hPTHR1-delNT, and also enhances the phospholipase C activity (EC50=17 μM).
| Molecular Weight | 635.65 |
| Formula | C29H32F3N5O6S |
| CAS Number | 1613373-33-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 95 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related Thyroid Hormone Receptor Products |
|---|
| ZYT-1
ZYT-1 is a thyroid receptor (THR-β) agonist. |
| VK-0214
VK-0214 is an orally active, selective small molecule agonist of the thyroid receptor (THR-β) for studies related to X-linked adrenoleukodystrophy (X-ALD) and hyperlipidemia. |
| PF-00277343
PF-00277343 is a selective thyroid receptor (THR-β) agonist. |
| Parathyroid Hormone (1-34), bovine
Parathyroid Hormone (1-34), bovine is a potent parathyroid hormone (PTH) receptor agonist. |
| (D-Trp12, Tyr34)-pTH (7-34) amide (bovine)
(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
