SC 57461A
- Product Name
- SC 57461A
- CAS No.
- 423169-68-0
- Chemical Name
- SC 57461A
- Synonyms
- SC 57461;SC 57461A;SC-57461 Hydrochloride;N-methyl-N-[3-[4-(phenylmethyl)phenoxy]propyl]-β-alaninehydrochloride;3-((3-(4-Benzylphenoxy)propyl)(methyl)amino)propanoic acid hydrochloride;inhibit,SC57461A,SC 57461A,Leukotriene A4,SC-57461A,Inhibitor,Aminopeptidase,orally active,LTA4 hydrolase
- CBNumber
- CB72446539
- Molecular Formula
- C20H25NO3.ClH
- Formula Weight
- 363.882
- MOL File
- 423169-68-0.mol
SC 57461A Property
- Melting point:
- 163-165°C
- storage temp.
- Desiccate at +4°C
- solubility
- DMSO: >5mg/mL
- form
- powder
- color
- white to off-white
Safety
- Hazard Codes
- Xn
- Risk Statements
- 22-36/37/38
- Safety Statements
- 26
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- PZ0110
- Product name
- SC-57461A
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $147
- Updated
- 2024/03/01
- Product number
- PZ0110
- Product name
- SC-57461A
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $461
- Updated
- 2024/03/01
- Product number
- 10108
- Product name
- SC-57461A
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 10108
- Product name
- SC-57461A
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 10108
- Product name
- SC-57461A
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
SC 57461A Chemical Properties,Usage,Production
Description
Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro. SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM). It blocks both the hydrolase and aminopeptidase activity in vitro. SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 or 6-keto prostaglandin F1α production . Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.
Chemical Properties
White Solid
Uses
SC 57461A is a potent and selective inhibitor of LTA4.
Uses
A potent and selective orally active leukotriene A4 hydrolase inhibitor.
Biological Activity
Potent and selective inhibitor of LTA 4 hydrolase. Does not inhibit other enzymes of the arachidonic acid cascade including COX-1, COX-2, LTC 4 synthase and 5-lipoxygenase. Potently inhibits LTB 4 production in whole blood (IC 50 = 49 nM). Orally active.
in vivo
SC-57461A also shows excellent potency in the mouse ex vivo assay, inhibiting the production of LTB4 with an ED50=0.2 mg/kg and an ED90=1 mg/kg. SC-57461A also inhibits the production of LTB4 in the rat peritoneal model with an ED50=1 mg/kg[2]. SC-57461A is a potent, selective, and competitive inhibitor of LTA4 hydrolase with excellent activity in whole animals. SC-57461A demonstrates good oral activity in both the mouse and the rat[3].
| Animal Model: | Fasted CD rats[3] |
| Dosage: | 0.01, 0.1, 1, and 10 mg/kg |
| Administration: | Orally administered |
| Result: | The ED50 values were 0.2 mg/kg at 1.0 h and 0.8 mg/kg at 3.0 h. A single dose of 10 mg/kg blocked LTB4 production 79% at 6 h, 67% at 18 h, and 44% at 24 h. |
References
[1] THOMAS D. PENNING. Synthesis of Potent Leukotriene A4 Hydrolase Inhibitors. Identification of 3-[Methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic Acid[J]. Journal of Medicinal Chemistry, 2002, 45 16: 3482-3490. DOI: 10.1021/jm0200916
[2] KACHUR J, ASKONAS L J, VILLANI-PRICE D, et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase II: in vivo studies.[J]. The Journal of Pharmacology and Experimental Therapeutics, 2002, 20 1: 0. DOI: 10.1124/jpet.300.2.583
[3] KACHUR J, ASKONAS L J, VILLANI-PRICE D, et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase II: in vivo studies.[J]. The Journal of Pharmacology and Experimental Therapeutics, 2002, 20 1: 0. DOI: 10.1124/jpet.300.2.583
SC 57461A Preparation Products And Raw materials
Raw materials
Preparation Products
SC 57461A Suppliers
- Tel
- --
- Fax
- --
- info@trc-canada.com
- Country
- Canada
- ProdList
- 6038
- Advantage
- 71