1400W dihydrochloride |
| Katalog-Nr.GC13563 |
1400 W Dihydrochlorid ist ein potenter und selektiver Inhibitor der humanen induzierbaren NO-Synthase mit Ki-Werten von 7 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 214358-33-5
Sample solution is provided at 25 µL, 10mM.
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1400W dihydrochloride is a potent and selective inhibitor of inducible nitric oxide synthase with Kd value of 7 nM [1].
Inducible nitric oxide synthase (iNOS) is an enzyme catalyzing the production of nitric oxide (NO) and is involved in immune response. iNOS produces NO as an immune defense mechanism.
1400W dihydrochloride is an extremely slowly reversible and selective iNOS inhibitor [1]. 1400W inhibited iNOS with Kd value of 7 nM and rapidly reversibly inhibited human neuronal NOS (nNOS) and endothelial NOS (eNOS) with Ki values of 2 and 50 μM, respectively. L-arginine was a competitive inhibitor of 1400W with Ks value of 3.0 μM [1].
In an endotoxin-induced vascular injury rat model, 1400W exhibited 50-fold more potent selectivity against iNOS than eNOS [1]. In focal cerebral ischaemia rats, 1400W (20 mg/kg) inhibited neurological dysfunction and weight loss and significantly decreased ischaemic lesion volume by 31%. Also, 1400W reduced iNOS activity by 36% in the infarct [2]. In the EMT6 murine mammary adenocarcinoma, 1400W (10 or 12 mg/kg/h) significantly reduced tumor weight and inhibited iNOS activity [3].
References:
[1]. Garvey EP, Oplinger JA, Furfine ES, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem, 1997, 272(8): 4959-4963.
[2]. Thomsen LL, Scott JM, Topley P, et al. Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor. Cancer Res, 1997, 57(15): 3300-3304.
[3]. Parmentier S, Böhme GA, Lerouet D, et al. Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. Br J Pharmacol, 1999, 127(2): 546-552.
| Kinase experiment [1]: | |
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Kinase assays |
The oxidation of L-[14C]arginine was monitored by the conversion of L-[14C]arginine to L-[14C]citrulline. The enzyme was assayed at 37°C in 20 mM Hepes, pH 7.4, with 2.5 mM dithiothreitol, 125 μM NADPH, 10 μM tetrahydrobiopterin, 10 μM FAD, and 0.5-20 μM L-[14C]arginine (10,000 cpm). When eNOS or nNOS were assayed, calmodulin (10 μg/ml) and CaCl2 (2.5 mM) were included. When time courses were measured, bovine serum albumin (1 mg/ml) was included. |
| Animal experiment [1]: | |
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Animal models |
Rat model of endotoxin-induced microvascular injury |
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Dosage form |
0.1-10 mg/kg, subcutaneous |
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Application |
1400W was a potent inhibitor against iNOS in a rat model of endotoxin-induced vascular injury. When administered 3 h after endotoxin, 1400W completely suppressed leakage into the ileum. 1400W has an effect of endotoxin -induced vascular injury in the ileum. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Garvey EP, Oplinger JA, Furfine ES, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem, 1997, 272(8): 4959-4963. | |
| Cas No. | 214358-33-5 | SDF | |
| Chemical Name | (E)-N'-(3-(aminomethyl)benzyl)acetimidamide dihydrochloride | ||
| Canonical SMILES | NCC1=CC(C/N=C(C)/N)=CC=C1.Cl.Cl | ||
| Formula | C10H15N3.2HCl | M.Wt | 250.17 |
| Löslichkeit | ≥ 25mg/mL in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9973 mL | 19.9864 mL | 39.9728 mL |
| 5 mM | 0.7995 mL | 3.9973 mL | 7.9946 mL |
| 10 mM | 0.3997 mL | 1.9986 mL | 3.9973 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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