1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor

JNJ-10229570 

Cat. No.: HY-107139 Purity: >98.0%
Handling Instructions

JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.

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

JNJ-10229570 Chemical Structure

JNJ-10229570 Chemical Structure

CAS No. : 524923-88-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.

IC50 & Target

IC50: 270 nM (human MC1R), 200 nM (human MC5R)[1].

In Vitro

JNJ-10229570 dose dependently inhibits the production of sebaceous lipids in cultured primary human sebocytes. JNJ-7818369 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50s of 270±120 and 200±50 nM, respectively. Nearly-identical results are obtained with the free base form of the compound. Binding to MC4R of both forms of the compound is equipotent, with IC50s of 240±170 nM. JNJ-10229570-treated cells show strong inhibition of lipid granules at 0.01 μM, and complete inhibition at 0.05 μM[1].

In Vivo

Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice result in a marked decrease in sebum-specific lipid production, sebaceous gland's size and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Topical treatment with 0.05% JNJ-10229570 leads to a distinct reduction in both the steady-state and the newly-synthesized sebum-specific lipids, with lesser effects on triglycerides and cholesterol[1].

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (160.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5676 mL 12.8380 mL 25.6759 mL
5 mM 0.5135 mL 2.5676 mL 5.1352 mL
10 mM 0.2568 mL 1.2838 mL 2.5676 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

References
Animal Administration
[1]

Mice[1]
Human skins transplanted onto SCID mice are topically treated with vehicle or JNJ-10229570 (0.05%) for 30 days[1].

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

References
Molecular Weight

389.47

Formula

C₂₂H₁₉N₃O₂S

CAS No.

524923-88-4

SMILES

COC1=C(C=CC=C1)C(N(C2=C(C=CC=C2)OC)S/3)=NC3=N\C4=CC=CC=C4

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

Room temperature in continental US; may vary elsewhere

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Product Name:
JNJ-10229570
Cat. No.:
HY-107139
Quantity:

JNJ-10229570

Cat. No.: HY-107139