| Size | Price | Stock | Qty |
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| 5mg |
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Zelnecirnon (RPT-193; RPT193) is a novel and potent inhibitor of CCR4 with anti-inflammatory activity and may be used for allergic inflammation in atopic dermatitis, and asthma. It acts by inhibiting the recruitment of Th2 inflammatory immune cells into inflamed tissues.
| ln Vitro |
Zelnecirnon has an IC50 of about 370 nM and inhibits Th2 cell chemotaxis or migration at concentrations of 1 nM–10 μM[2].
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|---|---|
| ln Vivo |
A mouse model of acute ovalbumin (OVA)-induced atopic dermatitis has shown that zelnecirnon (100 mg/kg; oral; once daily; 2 days, 1 day before OVA challenge) reduces skin inflammation [2].
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| Animal Protocol |
Animal/Disease Models: Mouse acute ovalbumin (OVA)-induced atopic dermatitis model [2]
Doses: 100 mg/kg Route of Administration: po (oral gavage); one time/day; lasts for 2 days, starting 1 day before OVA challenge (In mouse ears) Experimental Results: Significant reduction in ear thickness. |
| References |
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| Molecular Formula |
C27H34CL3N5O2
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|---|---|
| Molecular Weight |
566.95
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| Exact Mass |
565.177
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| CAS # |
2366152-15-8
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| PubChem CID |
139344142
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| Appearance |
White to off-white solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
811
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| Defined Atom Stereocenter Count |
2
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| SMILES |
[C@]1(C)(C(O)=O)C[C@@H](N2CCC[C@H](C3CN(C4=NC(C)=C(Cl)C(N[C@@H](C5=CC=C(Cl)C=C5Cl)C)=N4)C3)C2)C1
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| InChi Key |
ANPSFQZLPNWKHR-BPZFHHOVSA-N
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| InChi Code |
InChI=1S/C27H34Cl3N5O2/c1-15(21-7-6-19(28)9-22(21)29)31-24-23(30)16(2)32-26(33-24)35-13-18(14-35)17-5-4-8-34(12-17)20-10-27(3,11-20)25(36)37/h6-7,9,15,17-18,20H,4-5,8,10-14H2,1-3H3,(H,36,37)(H,31,32,33)/t15-,17+,20-,27-/m1/s1
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| Chemical Name |
(1R,3r)-3-((R)-3-(1-(5-chloro-4-(((R)-1-(2,4-dichlorophenyl)ethyl)amino)-6-methylpyrimidin-2-yl)azetidin-3-yl)piperidin-1-yl)-1-methylcyclobutane-1-carboxylic acid
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| Synonyms |
RPT-193 RPT193 ZelnecirnonRPT 193
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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 : ~100 mg/mL (~176.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7638 mL | 8.8191 mL | 17.6382 mL | |
| 5 mM | 0.3528 mL | 1.7638 mL | 3.5276 mL | |
| 10 mM | 0.1764 mL | 0.8819 mL | 1.7638 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.
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