| 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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| Other Sizes |
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| ln Vitro |
Vidupiprant (AMG 853, Compound 2) has a Kb of 0.2 nM and inhibits the downregulation of CRTH2 on CD16-negative granulocytes (eosinophils) in human whole blood caused by prostaglandin D2 (PGD2). Additionally, at a Kb of 4.7 nM, vidupiprant significantly reduced the PGD2-induced cAMP responses in human whole blood platelets by 80%, in contrast to AMG 009's Kb of 148 nM. Additionally, Vidupiprant was compared to the CRTH2 receptor downregulation human whole blood assay in the aequorin assay utilizing CRTH2-transfected HEK 293 cells and the eosinophil shape change assay [1].
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| ln Vivo |
In a guinea pig model of PGD2-induced airway constriction, Vidupiprant (AMG 853, Compound 2) showed much higher DP potency in vivo compared to AMG 009. Based on the PGD2 challenge, airway resistance is calculated in this model. The guinea pig whole blood cAMP assay was used to evaluate the in vitro DP potency. AMG 009 has a Kb of 82 nM, compared to 5 nM for Vidupiprant[1].
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| References | |
| Additional Infomation |
Vidupiprant has been used in trials studying the treatment and basic science of Asthma.
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| Molecular Formula |
C28H27CL2FN2O6S
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|---|---|
| Molecular Weight |
609.4904
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| Exact Mass |
608.095
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| CAS # |
1169483-24-2
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| PubChem CID |
42641863
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| Appearance |
White to off-white solid powder
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| LogP |
8.303
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PFWVGKROPKKEDW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H27Cl2FN2O6S/c1-28(2,3)32-27(36)17-6-8-23(39-24-14-21(31)18(11-19(24)29)13-26(34)35)22(12-17)33-40(37,38)25-9-7-16(10-20(25)30)15-4-5-15/h6-12,14-15,33H,4-5,13H2,1-3H3,(H,32,36)(H,34,35)
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| Chemical Name |
2-[4-[4-(tert-butylcarbamoyl)-2-[(2-chloro-4-cyclopropylphenyl)sulfonylamino]phenoxy]-5-chloro-2-fluorophenyl]acetic acid
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| Synonyms |
AMG-853; AMG 853; AMG853
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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 (~164.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.10 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6407 mL | 8.2036 mL | 16.4072 mL | |
| 5 mM | 0.3281 mL | 1.6407 mL | 3.2814 mL | |
| 10 mM | 0.1641 mL | 0.8204 mL | 1.6407 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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