| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
EC50: 0.41 nM (human FPR2), 3.4 nM (mouse FPR2), 2800 nM (human FPR1)[1]
|
|---|---|
| ln Vitro |
In order to promote the resolution of inflammation, BMS-986235 (LAR-1219) inhibits neutrophil chemotaxis and increases macrophage phagocytosis [1].
|
| ln Vivo |
Following the left anterior descending artery (LAD) in mice, BMS-986235 (LAR-1219) (0.3 mg/kg; oral; once daily for 24 days) decreases left ventricular and overall cardiac remodeling[1]. Cmax, T1/2, AUC0-inf, and bioavailability (BA) values of 160 nmol/L, 0.68 h, and 120 nmol/L were observed with BMS-986235 (1 mg/kg; po) therapy.h, and 24%, in that order[1].
|
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice[1]
Doses: 0.3 mg/kg Route of Administration: Po; daily for 24 days Experimental Results: Left ventricle (LV) chamber remodeling is attenuated after myocardial infarction (MI). decreased infarct length by 39% relative to vehicle. Animal/Disease Models: Male mice (BALB/cCrSlc)[1] Doses: 1 mg/kg Route of Administration: Po (pharmacokinetic/PK Analysis) Experimental Results: The Cmax, T1/2, AUC0-inf, and bioavailability (BA) values were 160 nmol/L, 0.68 hrs (hours), 120 nmol/L·h, and 24%, respectively. |
| References |
| Molecular Formula |
C18H17F2N3O3
|
|---|---|
| Molecular Weight |
361.34269118309
|
| Exact Mass |
361.123
|
| CAS # |
2253947-47-4
|
| PubChem CID |
122583088
|
| Appearance |
White to off-white solid powder
|
| LogP |
2
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
504
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
N([C@H]1[C@H](C2=C(F)C=C(OC)C=C2F)CNC1=O)C(NC1=CC=CC=C1)=O
|
| InChi Key |
FJZNNKJZHQFMCK-LRDDRELGSA-N
|
| InChi Code |
InChI=1S/C18H17F2N3O3/c1-26-11-7-13(19)15(14(20)8-11)12-9-21-17(24)16(12)23-18(25)22-10-5-3-2-4-6-10/h2-8,12,16H,9H2,1H3,(H,21,24)(H2,22,23,25)/t12-,16-/m0/s1
|
| Chemical Name |
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-phenylurea
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (276.75 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.92 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 (6.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 1.2 mg/mL (3.32 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7675 mL | 13.8374 mL | 27.6748 mL | |
| 5 mM | 0.5535 mL | 2.7675 mL | 5.5350 mL | |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7675 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
