2. GPCR/G Protein
  3. LPL Receptor
  4. Etrasimod

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

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Etrasimod

Etrasimod Estructura química

No. CAS : 1206123-37-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Etrasimod:

Etrasimod Related Antibodies

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1 Publications Citing Use of MCE Etrasimod

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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Descripciòn

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

IC50 & Target

IC50: 1.88 nM (S1P1)[1]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
1.88 nM
Compound: (R)-4, APD334
Induction of internalization of HA-tagged human S1P1 receptor expressed in CHO cells
Induction of internalization of HA-tagged human S1P1 receptor expressed in CHO cells
[PMID: 25516790]
THP-1 CC50
57.7 μM
Compound: 1; Etra
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin staining based analysis
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin staining based analysis
[PMID: 37948883]
In Vitro

APD334 is a structurally novel, selective, functional antagonist of S1P1. In CHO cells expressing HA tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P1 activity is maintained in mice (EC50=0.44 nM), rats (EC50=0.32 nM), dogs (EC50=0.34 nM) and monkeys (EC50=0.32 nM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Etrasimod Related Antibodies
In Vivo

APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmax across all species. In both dog and monkey a significant decrease in volume of distribution (Vss) is observed relative to rodent. Oral bioavailability is in the range of 40–100%, and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in dog. Rat and monkey t1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

457.48

Fòrmula

C26H26F3NO3
No. CAS
Appearance

Solid

Color

White to khaki

SMILES

FC(F)(F)C1=CC(COC2=CC=C(NC3=C4CC[C@@H]3CC(O)=O)C4=C2)=CC=C1C5CCCC5
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 116.67 mg/mL (255.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1859 mL 10.9294 mL 21.8589 mL
5 mM 0.4372 mL 2.1859 mL 4.3718 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.91%

SDS (393 KB)

COA (248 KB) LCMS (97 KB)

Instrucciones de manejo (2659 KB)
Referencias
Administraciòn de animales
[1]

Rats: APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose[1].

Mice: APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose[1].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1859 mL 10.9294 mL 21.8589 mL 54.6472 mL
5 mM 0.4372 mL 2.1859 mL 4.3718 mL 10.9294 mL
10 mM 0.2186 mL 1.0929 mL 2.1859 mL 5.4647 mL
15 mM 0.1457 mL 0.7286 mL 1.4573 mL 3.6431 mL
20 mM 0.1093 mL 0.5465 mL 1.0929 mL 2.7324 mL
25 mM 0.0874 mL 0.4372 mL 0.8744 mL 2.1859 mL
30 mM 0.0729 mL 0.3643 mL 0.7286 mL 1.8216 mL
40 mM 0.0546 mL 0.2732 mL 0.5465 mL 1.3662 mL
50 mM 0.0437 mL 0.2186 mL 0.4372 mL 1.0929 mL
60 mM 0.0364 mL 0.1822 mL 0.3643 mL 0.9108 mL
80 mM 0.0273 mL 0.1366 mL 0.2732 mL 0.6831 mL
100 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5465 mL
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Etrasimod Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Etrasimod1206123-37-6APD334APD 334APD-334LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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Nombre del producto:
Etrasimod
Cat. No.:
HY-12789
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