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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 157 In-stock
Solution
10 mM * 1 mL in DMSO USD 157 In-stock
Solid
5 mg USD 143 In-stock
10 mg USD 253 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CLP-3094

WB

    CLP-3094 purchased from MedChemExpress. Usage Cited in: Obesity. 2023 Mar 30.  [Abstract]

    CLP-3094 (CLP; 0.7 μM; 48 h) inhibits the PA (palmitic acid) increased expression of PDX-1, NKX6.1, and MAFA in MIN6 cells. whereas L-Trp (0.7 mM; 48 h) causes an opposing effect.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

    MedChemExpress (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].

    MedChemExpress (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

    Formula

    C15H13ClN2OS

    CAS No.
    Appearance

    Solid

    Color

    Off-white to brown

    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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2809 mL 16.4047 mL 32.8095 mL 82.0237 mL
    5 mM 0.6562 mL 3.2809 mL 6.5619 mL 16.4047 mL
    10 mM 0.3281 mL 1.6405 mL 3.2809 mL 8.2024 mL
    15 mM 0.2187 mL 1.0936 mL 2.1873 mL 5.4682 mL
    20 mM 0.1640 mL 0.8202 mL 1.6405 mL 4.1012 mL
    25 mM 0.1312 mL 0.6562 mL 1.3124 mL 3.2809 mL
    30 mM 0.1094 mL 0.5468 mL 1.0936 mL 2.7341 mL
    40 mM 0.0820 mL 0.4101 mL 0.8202 mL 2.0506 mL
    50 mM 0.0656 mL 0.3281 mL 0.6562 mL 1.6405 mL
    60 mM 0.0547 mL 0.2734 mL 0.5468 mL 1.3671 mL
    80 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0253 mL
    100 mM 0.0328 mL 0.1640 mL 0.3281 mL 0.8202 mL
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    CLP-3094 Related Classifications

    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
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