[CAS NO. 1613373-33-3]  PCO371

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PRODUCTS SPECIFICATIONS [1613373-33-3]

Catalog
HY-100856
Brand
MCE
CAS
1613373-33-3

DESCRIPTION [1613373-33-3]

Overview

MDL-
Molecular Weight635.65
Molecular FormulaC29H32F3N5O6S
SMILESFC(F)(F)OC1=CC=C(C2=NC3(CCN(S(CCC4=C(C)C=C(N5C(NC(C5(C)C)=O)=O)C=C4C)(=O)=O)CC3)C(N2)=O)C=C1

For research use only. We do not sell to patients.

Summary

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1) , with no effect on PTH type 2 receptor.


IC50 & Target

PTHR1 [1]


In Vitro

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor. PCO371 induces cAMP production with an EC 50 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 (EC 50 , 17 μM) [1] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02475616 Chugai Pharmaceutical
Healthy
June 2015 Phase 1
NCT04209179 Chugai Pharmaceutical
Hypoparathyroidism
July 23, 2020 Phase 1
NCT04649216 Chugai Pharmaceutical
Healthy Volunteers
November 25, 2020 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 196.65 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5732 mL 7.8660 mL 15.7319 mL
5 mM 0.3146 mL 1.5732 mL 3.1464 mL
10 mM 0.1573 mL 0.7866 mL 1.5732 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 6.25 mg/mL (9.83 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (9.83 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 6.25 mg/mL (9.83 mM); Clear solution

* All of the co-solvents are available by MCE.