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Purity: ≥98%
JNJ-10229570 is a novel, potent and selective antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R) with the potential to treat primary human sebaceous cells and for the treatment of acne and other sebaceous gland pathologies. JNJ-10229570 inhibits the lipid synthesis specific to sebum as well as the differentiation of sebaceous glands. Using IC50 values of 200 nM and 270 nM, respectively, JNJ-10229570 suppresses 125I-NDP-α-MSH binding to human MC1R and MC5R-expressing cells.
| Targets |
human MC1R ( IC50 = 270 nM ); human MC5R ( IC50 = 200 nM )
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|---|---|
| ln Vitro |
JNJ-10229570 inhibits the synthesis of sebaceous lipids in cultured primary human sebocytes in a dose-dependent manner. At IC50s of 270±120 and 200±50 nM, respectively, JNJ-7818369 inhibits the binding of 125I-NDP-α-MSH to human MC1R and MC5R expressing cells. The compound's free base form yields almost identical results. Both forms of the compound bind to MC4R equipotently, with IC50 values of 240±170 nM. Lipid granules are strongly inhibited in cells treated with JNJ-10229570 at 0.01 μM and completely inhibited at 0.05 μM [1].
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| ln Vivo |
Topical application of JNJ-10229570 from human skins transplanted onto SCID mice leads to a significant reduction in the production of lipids specific to sebum, the size of the sebaceous glands, and the expression of the marker of sebaceous differentiation, epithelial-membrane antigen (EMA). Topical application of 0.05% JNJ-10229570 causes a noticeable decrease in newly-synthesised and steady-state sebum-specific lipids, while having less of an impact on cholesterol and triglycerides[1].
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| Animal Protocol |
Mice: JNJ-10229570 (0.05%) or vehicle is topically applied for 30 days after human skin transplants onto SCID mice[1].
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| References |
| Molecular Formula |
C22H19N3O2S
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|---|---|
| Molecular Weight |
389.470163583755
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| Exact Mass |
389.12
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| Elemental Analysis |
C, 67.84; H, 4.92; N, 10.79; O, 8.22; S, 8.23
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| CAS # |
524923-88-4
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| Appearance |
Solid powder
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| SMILES |
COC1=CC=CC=C1C2=NC(=NC3=CC=CC=C3)SN2C4=CC=CC=C4OC
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| InChi Key |
XTHRTBCPBWJYRO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19N3O2S/c1-26-19-14-8-6-12-17(19)21-24-22(23-16-10-4-3-5-11-16)28-25(21)18-13-7-9-15-20(18)27-2/h3-15H,1-2H3
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| Chemical Name |
2,3-bis(2-methoxyphenyl)-N-phenyl-1,2,4-thiadiazol-5-imine
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| Synonyms |
JNJ 10229570; JNJ-10229570; JNJ10229570; UNII-N9IX402L35
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 62.5~78 mg/mL (160.5~200.3 mM
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01492647 | Completed | Drug: JNJ 10229570-AAA 1.2% Drug: JNJ 10229570-AAA 3.6% |
Acne Vulgaris | Janssen Pharmaceutical K.K. | August 2011 | Phase 1 |
| NCT01494714 | Completed | Drug: JNJ 10229570-AAA 1.2% cream Drug: Petroleum jelly |
Healthy Volunteers | Janssen Pharmaceutical K.K. | August 2011 | Phase 1 |
| NCT01326780 | Completed | Drug: 1.2% JNJ 10229570-AAA Drug: 2.4% JNJ 10229570-AAA |
Acne Vulgaris | Bausch Health Americas, Inc. | March 31, 2011 | Phase 2 |
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