| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
Similar to how recombinant human TPO (rhTPO) does, avatrombopag (E5501; AKR-501) hydrochloride selectively targets the TPO receptor and stimulates megakaryocytopoiesis throughout the growth and maturation of megakaryocytes. It has been demonstrated that avatrombopag hydrochloride exclusively affects humans and chimpanzees[1]. In a concentration-dependent manner, avatrombopag hydrochloride (0-100 nM) promotes the growth of Ba/F3 cells that express TPO receptors. In the cells, avatrombopag hydrochloride (0-3 μM) and rhTPO both cause tyrosine phosphorylation of STAT3 and STAT5, as well as threonine phosphorylation of ERK[1]. Megakaryocyte colony formation from human CB CD34+ cells is promoted by avatrombopag hydrochloride in a concentration-dependent manner. For Avatrombopag hydrochloride, the EC50 is 25 nM, and its maximal activity is comparable to that of rhTPO[1].
|
|---|---|
| ln Vivo |
In NOD/SCID mice transplanted with human FL CD34+ cells, avatrombopag hydrochloride (0.3-3 mg/kg; po; daily for 14 days) enhances the amount of human platelets[1].
|
| Animal Protocol |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse (transplanted with human FL CD34+cells)[1]
Doses: 0.3, 1, and 3 mg/kg Route of Administration: Po; daily for 14 days Experimental Results: Dose-dependently increased the number of human platelets, resulting in approximately a 2.7-fold increase at 1 mg/ kg/d and a 3.0-fold increase at 3 mg/kg/d on day 14 after the start of administration. |
| References |
|
| Molecular Formula |
C29H35CL3N6O3S2
|
|---|---|
| Molecular Weight |
686.1156
|
| Exact Mass |
684.127
|
| CAS # |
570403-17-7
|
| Related CAS # |
Avatrombopag;570406-98-3;Avatrombopag maleate;677007-74-8;Avatrombopag-d8 hydrochloride
|
| PubChem CID |
87588882
|
| Appearance |
Off-white to gray solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
43
|
| Complexity |
935
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C([H])=C(C([H])=NC=1N1C([H])([H])C([H])([H])C([H])(C(=O)O[H])C([H])([H])C1([H])[H])C(N([H])C1=NC(C2=C([H])C(=C([H])S2)Cl)=C(N2C([H])([H])C([H])([H])N(C([H])([H])C2([H])[H])C2([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C2([H])[H])S1)=O.Cl[H]
|
| InChi Key |
JSHJSCRYBTVFTI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C29H34Cl2N6O3S2.ClH/c30-20-15-23(41-17-20)24-27(37-12-10-35(11-13-37)21-4-2-1-3-5-21)42-29(33-24)34-26(38)19-14-22(31)25(32-16-19)36-8-6-18(7-9-36)28(39)40;/h14-18,21H,1-13H2,(H,39,40)(H,33,34,38);1H
|
| Chemical Name |
1-[3-chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)-1,3-thiazol-2-yl]carbamoyl]pyridin-2-yl]piperidine-4-carboxylic acid;hydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 8.33 mg/mL (12.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.21 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 8.3 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 | 1.4575 mL | 7.2874 mL | 14.5747 mL | |
| 5 mM | 0.2915 mL | 1.4575 mL | 2.9149 mL | |
| 10 mM | 0.1457 mL | 0.7287 mL | 1.4575 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
