2. GPCR/G Protein
  3. Platelet-activating Factor Receptor (PAFR)
  4. Apafant

Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit.

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Apafant Chemical Structure

Apafant Chemical Structure

CAS No. : 105219-56-5

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Based on 1 publication(s) in Google Scholar

Apafant Related Antibodies

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Description

Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit[1][2][3].

IC50 & Target

Ki: 9.9 nM (Platelet-activating factor)[1]
In Vitro

Apafant (1 mM; 5 days) increases the gene expression of PAF-r, α-globin, β-globin, and decreases the c-myb gene expression in murine erythroleukemia cells (MELCs)[2].

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

Apafant Related Antibodies

RT-PCR[2]

Cell Line: Murine erythroleukemia cells (MELCs)
Concentration: 1 mM
Incubation Time: 5 days
Result: Iecreased the gene expression of PAF-r, α-globin, β-globin, decreased the c-myb gene expression.
In Vivo

Apafant (1, 5, 10, 20, 30 mg/kg) shows a protective effect on alkyl-PAF-mediated lethality in Swiss albino mice[3].

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

Animal Model: 20-25 g, Swiss albino mice[3]
Dosage: 1, 5, 10, 20, 30 mg/kg (3 h later, challenged with a lethal dose of alkyl-PAF (250 μg/kg); ip)
Administration: IP; once
Result: Increased mouse survival with none of the mice died when they were pretreated with WEB-2086 and then challenged with a lethal dose of alkyl-PAF 5 h later, Only 17% died when challenged 10 h after the WEB-2086 pretreatment. Even in the groups that received the alkyl-PAF injection 30 or 45 h after the WEB-2086 pretreatment, 33% of the mice still survived.
Molecular Weight

455.96

Formula

C22H22ClN5O2S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(N1CCOCC1)CCC(S2)=CC3=C2N4C(CN=C3C5=CC=CC=C5Cl)=NN=C4C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (87.73 mM; Need ultrasonic and warming; 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 2.1932 mL 10.9659 mL 21.9317 mL
5 mM 0.4386 mL 2.1932 mL 4.3863 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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
Purity & Documentation

Purity: 99.96%

SDS (419 KB)

COA (257 KB) LCMS (96 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1932 mL 10.9659 mL 21.9317 mL 54.8294 mL
5 mM 0.4386 mL 2.1932 mL 4.3863 mL 10.9659 mL
10 mM 0.2193 mL 1.0966 mL 2.1932 mL 5.4829 mL
15 mM 0.1462 mL 0.7311 mL 1.4621 mL 3.6553 mL
20 mM 0.1097 mL 0.5483 mL 1.0966 mL 2.7415 mL
25 mM 0.0877 mL 0.4386 mL 0.8773 mL 2.1932 mL
30 mM 0.0731 mL 0.3655 mL 0.7311 mL 1.8276 mL
40 mM 0.0548 mL 0.2741 mL 0.5483 mL 1.3707 mL
50 mM 0.0439 mL 0.2193 mL 0.4386 mL 1.0966 mL
60 mM 0.0366 mL 0.1828 mL 0.3655 mL 0.9138 mL
80 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6854 mL
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Apafant Related Classifications

Help & FAQs
  • 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:

Apafant105219-56-5WEB 2086WEB2086WEB-2086Platelet-activating Factor Receptor (PAFR)PAF-rα-globinβ-globinc-mybMELCalkyl-PAFInhibitorinhibitorinhibit

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