Etrasimod
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 50mg | $650 | Check With Us |
| 100mg | $950 | Check With Us |
| 200mg | $1425 | Check With Us |
: Cat #: V20842 CAS #: 1206123-37-6 Purity ≥ 98%
Description: Etrasimod (formerly APD334; APD3-34) is a potent, centrally bioavailable, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases.
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| Molecular Weight (MW) | 457.48 |
|---|---|
| Molecular Formula | C26H26F3NO3 |
| CAS No. | 1206123-37-6 |
| Protocol | In Vitro | The APD334 is a novel, selective, and functional S1P1 Antagonists. S1P expressing the HA tag1 The IC of APD334 was found in CHO cells50 The value is 1.88 nM. Observed in human S1P4 and S1P5 but lower than S1P in potency and efficacy1。 APD334 to Human S1P2 and S1P3 There is no agitation or antagonism. APD334 achieves good central exposure after oral administration and has a good pharmacokinetic profile in multiple preclinical species. S1P1Active in mice (EC50=0.44 nM), rat (EC50=0.32 nM), dog (EC>50=0.34 nM) and monkey (EC50=0.32 nM) |
|---|---|---|
| In Vivo | APD334 has relatively low systemic clearance (<4% hepatic blood flow) and high C in all species.max。 A significant decrease in volume of distribution (VSS) relative to rodents was observed in dogs and monkeys. Oral bioavailability is in the 40-100% range, with terminal half-lives ranging from 6 hours in monkeys to 29 hours in dogs. Siponimod (another S1P1 modulator currently undergoing human trials) in rats and monkeys1/2 The values are already publicly available, 6 and 19 hours, respectively |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1859 mL | 10.9294 mL | 21.8589 mL | 43.7178 mL |
| 5mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | 8.7436 mL |
| 10mM | 0.2186 mL | 1.0929 mL | 2.1859 mL | 4.3718 mL |
| 20mM | 0.1093 mL | 0.5465 mL | 1.0929 mL | 2.1859 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid 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 master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.