ChemicalBook Product Catalog API Antiallergic drugs Allergic Reactions Apafant

Apafant

Product NameApafant
CAS105219-56-5
MFC22H22ClN5O2S
MW455.96
EINECS
MOL File105219-56-5.mol

Chemical Properties

Melting point	186-188°C
Boiling point	720.2±70.0 °C(Predicted)
Density	1.48
storage temp.	2-8°C
solubility	DMSO: soluble10mg/mL (clear solution)
pka	2.36±0.40(Predicted)
form	powder
color	white to beige
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChI	1S/C22H22ClN5O2S/c1-14-25-26-19-13-24-21(16-4-2-3-5-18(16)23)17-12-15(31-22(17)28(14)19)6-7-20(29)27-8-10-30-11-9-27/h2-5,12H,6-11,13H2,1H3
InChIKey	JGPJQFOROWSRRS-UHFFFAOYSA-N
SMILES	Cc1nnc2CN=C(c3ccccc3Cl)c4cc(CCC(=O)N5CCOCC5)sc4-n12

Safety Information

WGK Germany	3
Storage Class	11 - Combustible Solids
Toxicity	LD50 in mice (mg/kg): 540 i.v.; 4600 orally (Casals-Stenzel)

Usage And Synthesis

Description

WEB-2086 (105219-56-5) is a potent and selective antagonist of the platelet activating factor (PAF) receptor (Ki = 16.3 nM).1Displays an activity profile which includes antiinflammatory, antiangiogenesis and anticancer activity.2Along with leukotriene antagonists, WEB-2086 cooperatively provides a robust antiinflammatory effect regulating PMNL migration and edema formation.3Displays analgesic effects in animal models of neuropathic pain.4Active in vivo.

Chemical Properties

White Solid

Uses

Platelet activating factor (PAF) antagonist.

Uses

Tool to evaluate the role of PAF in experimental models of human disease.

Definition

ChEBI: LSM-2613 is an organonitrogen heterocyclic compound and an organosulfur heterocyclic compound.

Biological Activity

Potent, selective platelet-activating factor (PAF) receptor antagonist (K i = 16.3 nM). Displays anti-inflammatory, antiangiogenic and anticancer activity. Inhibits growth and proliferation of MCF-7 breast cancer cells.

Biochem/physiol Actions

WEB2086 is a very potent, selective platelet-activating factor (PAF) antagonist (IC50 = 16 nM). WEB2086 inhibits the proliferation of tumor cells and slows tumor growth in xenograft tumor models, and has been shown to inhibit angiogenesis.

storage

Desiccate at +4°C

References

[1] GORDON DENT . Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086 Correlation between receptor binding and function[J]. FEBS Letters, 1989, 244 2: Pages 365-368. DOI:10.1016/0014-5793(89)80564-2
[2] C CELLAI. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086[J]. British Journal of Cancer, 2006, 94 11: 1637-1642. DOI:10.1038/sj.bjc.6603156
[3] CLAUDIA S. BITENCOURT. Cooperative role of endogenous leucotrienes and platelet-activating factor in ischaemia–reperfusion-mediated tissue injury[J]. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE, 2013, 17 12: 1554-1565. DOI:10.1111/jcmm.12118
[4] N. MOTOYAMA. Pain-releasing action of Platelet-activating factor (PAF) antagonists in neuropathic pain animal models and the mechanisms of action[J]. European Journal of Pain, 2013, 17 8: 1156-1167. DOI:10.1002/j.1532-2149.2013.00289.x

Apafant

Chemical Properties

Safety Information

Usage And Synthesis

Preparation Products And Raw materials

Apafant Supplier

Apafant manufacturers

Related Product Information