GW311616A
- Product Name
- GW311616A
- CAS No.
- 197890-44-1
- Chemical Name
- GW311616A
- Synonyms
- CS-1260;GW 311616A;GW-311616A;GW 311616A - GW 311616 hydrochloride;GW311616 hydrochloride,GW-311616 hydrochloride
- CBNumber
- CB8498151
- Molecular Formula
- C19H32ClN3O4S
- Formula Weight
- 433.99
- MOL File
- 197890-44-1.mol
GW311616A Property
- storage temp.
- 2-8°C
- solubility
- H2O: 24 mg/mL, soluble
- form
- solid
- color
- White to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- 27957
- Product name
- GW 311616A
- Packaging
- 1mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 27957
- Product name
- GW 311616A
- Packaging
- 10mg
- Price
- $396
- Updated
- 2024/03/01
- Product number
- 27957
- Product name
- GW 311616A
- Packaging
- 5mg
- Price
- $238
- Updated
- 2024/03/01
- Product number
- Axon2364
- Product name
- GW311616A-GW311616hydrochloride
- Purity
- 99%
- Packaging
- 5mg
- Price
- $198
- Updated
- 2021/12/16
- Product number
- B4676
- Product name
- GW311616hydrochloride
- Packaging
- 100mg
- Price
- $210
- Updated
- 2021/12/16
GW311616A Chemical Properties,Usage,Production
Description
GW 311616A is an inhibitor of neutrophil elastase (IC50 = 100 nM). It is selective for neutrophil elastase (IC50 = 22 nM for the human enzyme) over trypsin, cathepsin G, and plasmin (IC50s = >100 μM for all), as well as chymotrypsin and tissue plasminogen activator (IC50s = >3 μM for both), in cell-free assays. GW 311616A (20 μM) inhibits the formation of neutrophil extracellular traps (NETs) induced by phorbol 12-myristate 13-acetate (PMA; ) in isolated human neutrophils. It inhibits intraneutrophil elastase activity in isolated dog blood six hours after administration of a 0.22 mg/kg dose. GW 311616A also inhibits neutrophil elastase in the liver in a mouse model of liver ischemia-reperfusion injury when administered at a dose of 2 mg/kg.
Uses
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM[1].
in vivo
GW-311616 (2 mg/kg; oral administration) rapidly abolishes the circulation of neutrophil elastase (NE) in dogs, while >90% inhibition is maintained for 4 days. This prolonged effect is independent to be due to penetration of neutrophils in bone marrow by orally administrated GW-311616. GW-311616 has moderate terminal elimination half-life (t1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively[3].
| Animal Model: | Dogs (9-month-old)[3] |
| Dosage: | 0.22 mg/kg, 0.66 mg/kg and 2 mg/kg (Pharmacokinetic study) |
| Administration: | Oral administration |
| Result: | At 0.22 mg/kg, greater than 50% inhibition of elastase is achieved 6 hours after dosing, with activity returning towards control values. Single oral dose of 2 mg/kg rapidly abolishes circulating enzyme activity, and greater than 90% inhibition is maintained for 4 days. |
References
[1] macdonald sj1, dowle md, harrison la, shah p, johnson mr, inglis gg, clarke gd, smith ra, humphreys d, molloy cr, amour a, dixon m, murkitt g, godward re, padfield t, skarzynski t, singh om, kumar ka, fleetwood g, hodgson st, hardy gw, finch h. the discovery of a potent, intracellular, orally bioavailable,long duration inhibitor of human neutrophil elastase-gw311616a a development candidate. bioorg med chem lett. 2001 apr 9;11(7):895-8.
GW311616A Preparation Products And Raw materials
Raw materials
Preparation Products
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