1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. CLP-3094

CLP-3094 

Cat. No.: HY-141487 Purity: ≥95.0%
COA Handling Instructions

CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.

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

CLP-3094 Chemical Structure

CLP-3094 Chemical Structure

CAS No. : 312749-73-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 157 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 157 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 143 In-stock
Estimated Time of Arrival: December 31
10 mg USD 253 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].

In Vitro

CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC50 of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists[2].

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

In Vivo

CLP-3094 (30, 100 mg/kg; i.p. daily from Day 0 to Day 11) consistently displayed sig-nificantly lower severity of arthritis scores than vehicletreated mice[2].

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

Animal Model: CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)[2]
Dosage: 30, 100 mg/kg
Administration: I.p. daily from Day 0 to Day 11
Result: Dose-dependently reduced, by not much, the arth-ritis scores.
Molecular Weight

304.79

Appearance

Solid

Formula

C15H13ClN2OS

CAS No.
SMILES

ClC1=CC=C(OCCSC2=NC3=CC=CC=C3N2)C=C1

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 : 100 mg/mL (328.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2809 mL 16.4047 mL 32.8095 mL
5 mM 0.6562 mL 3.2809 mL 6.5619 mL
10 mM 0.3281 mL 1.6405 mL 3.2809 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: ≥ 2.5 mg/mL (8.20 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.20 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Product Name:
CLP-3094
Cat. No.:
HY-141487
Quantity:
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