Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
Nerandomilast, with IC50 values of 35 nM, suppresses the release of IL-2 caused by phytohemagglutinin P (HY-N7038A) and TNF-α induced by lipopolysaccharides (HY-D1056) in human peripheral blood monolayer cells. and 9 nM [2]. With an IC50 value of 91 nM, nerandomilast suppresses TNF-α release in rat whole blood[2].
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ln Vivo |
In rats, nerandomilast (Example 2) at 1.0 mg/kg reduced intestinal transit without significantly altering body weight (0, 0.3, 1.0, and 3.0 mg/kg; oral; single dose)[1]. Nerandomilast has an ED50 value of 0.1 mg/kg and can reduce inflammation in rat lung tissue[1]. In a dose-dependent way, nerandomilast (0.01, 0.1, and 1.0 mg/kg; oral; single dose) decreases TNF-α release in mouse plasma produced by lipopolysaccharides (HY-D1056)[2]. Male Suncus Murinus and Wistar rats' bronchoalveolar lavage fluid is not affected by lipopolysaccharide-induced neutrophil entrance when nerandomilast (0.1, 0.3, and 1.0 mg/kg; oral; single dosage) is administered[2]. Nerandomilast (orally administered twice daily for six days at doses of 2.5 mg/kg and 12.5 mg/kg) significantly reduces bleomycin (HY-108345)-induced injury in mice[2].
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Animal Protocol |
Animal/Disease Models: Rats[1].
Doses: 0, 0.3, 1.0 and 3.0 mg/kg. Route of Administration: Oral gavage; single dose. Experimental Results: Had minimal toxic and side effects on the intestines and stomach of rats, demonstrating biosafety. Animal/Disease Models: Male Suncus Murinus and Wistar rats; mice[2]. Doses: 0.01, 0.1, 0.3, 1.0, 2.5 or 12.5 mg/kg. Route of Administration: Oral gavage; single dose or twice (two times) daily for 6 days. Experimental Results: Effectively improved inflammation in lung tissue and decreased the pro-inflammatory factor TNF-α release. |
References |
[1]. Pouzet P A, et al. Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma. United States. US9150586.
[2]. Herrmann FE, et al. BI 1015550 is a PDE4B Inhibitor and a Clinical Drug Candidate for the Oral Treatment of Idiopathic Pulmonary Fibrosis. Front Pharmacol. 2022 Apr 20;13:838449. |
Molecular Formula |
C20H25CLN6O2S
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Molecular Weight |
448.97
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CAS # |
1423719-30-5
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Related CAS # |
Nerandomilast dihydrate
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1C=NC(C2CCN(C3N=C4CC[S@](C4=C(N=3)NC3(CO)CCC3)=O)CC2)=NC=1
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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: 10 mg/mL (22.27 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (11.14 mM) 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; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2273 mL | 11.1366 mL | 22.2732 mL | |
5 mM | 0.4455 mL | 2.2273 mL | 4.4546 mL | |
10 mM | 0.2227 mL | 1.1137 mL | 2.2273 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.