ChemicalBook CAS DataBase List 125228-51-5

125228-51-5

Name	L 156602
CAS	125228-51-5
Molecular Formula	C38H64N8O13
MDL Number	MFCD00891644
Molecular Weight	840.961
MOL File	125228-51-5.mol

Chemical Properties

density	1.37±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: soluble; DMSO: soluble; Ethanol: soluble
form	A solid
pka	8.47±0.70(Predicted)

Hazard Information

Description

PD 124966 is a potent antitumor agent isolated from Streptomyces sp.; a cyclic hexadepsipeptide; antagonist of complement 5A.

Uses

L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH)[1][2].

in vivo

L-156602 (0.1-0.5 mg/kg, i.p., once daily for 3 days) suppressed inflammation significantly in CDF1 mice induced by Concanavalin A (HY-P2149) and BALB/c mice induced by Muramyl dipeptide (MDP) (HY-127090)^[1]^[2].
L-156602 (0.2-0.5 mg/kg, i.p.) suppressed the infiltration of mononuclear leukocytes and neutrophils into the site of inflammation in PCI-induced inflammation of DBA/1 mice^[2].

Animal Model:	Concanavalin A-induced inflammation of CDF1 mice^[1]^[2]
Dosage:	0.1, 0.5 mg/kg, once daily for 3 days
Administration:	Intraperitoneal injection (i.p.)
Result:	Suppressed the swelling completely after 4 h at 0.1 mg/kg, and the effect was still statistical after 24 h at 0.5 mg/kg. Reduced the number of migrated leukocytes. Suppressed the migration of neutrophils, macrophages and lymphocytes non-specifically.

Animal Model:	MDP-induced acute joint inflammation of BALB/c mice^[1]
Dosage:	0.25, 0.5 mg/kg, once daily for 3 days
Administration:	Intraperitoneal injection (i.p.)
Result:	Suppressed adjuvant arthritis although a slight reduction of body weight at the dose of 0.5 mg/kg after 24 h.

Animal Model:	0.5% PCI-induced inflammation of DBA/1 mice^[2]
Dosage:	0.2, 0.5 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Suppressed ear swelling significantly and the infiltration of mononuclear leukocytes and neutrophils into the site of inflammation.

Animal Model:	5% PCI-induced inflammation of DBA/1 mice^[2]
Dosage:	0.4 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Suppressed the infiltration of mononuclear leukocytes and neutrophils into the site of inflammation non-specifically.

References

[1] Tsuji RF, et al. Effects of L-156,602, a C5a receptor antagonist, on mouse experimental models of inflammation. Biosci Biotechnol Biochem. 1992 Dec;56(12):2034-6. DOI:10.1271/bbb.56.2034
[2] Tsuji RF, et al. Anti-inflammatory effects and specificity of L-156,602: comparison of effects on concanavalin A and zymosan-induced footpad edema, and contact sensitivity response. Immunopharmacology. 1995 Feb;29(1):79-87. DOI:10.1016/0162-3109(95)00047-w

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