| Identification | Back Directory | [Name]
L 156602 | [CAS]
125228-51-5 | [Synonyms]
Antibiotic L 16602
Antibiotic L 156602
ZJZOPNINWIGNQW-UHFFFAOYSA-N | [Molecular Formula]
C38H64N8O13 | [MDL Number]
MFCD00891644 | [MOL File]
125228-51-5.mol | [Molecular Weight]
840.961 |
| Chemical Properties | Back Directory | [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 | Back Directory | [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.
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| 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.
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| 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.
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| 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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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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