Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
ln Vitro |
During the day, oligodendrocytes' eIF2α phosphorylation is prolonged by cerguastat (5 μM) [1]. Holophosphatase phosphatase Icerguastat (Sephin1) selectively binds to and inhibits downstream-induced PPP1R15A, but not associated PPP1R15B, to prolong phosphosignal coupling Supplement and prevent other proteins' misfolded middle section from undergoing apoptosis [2].
|
---|---|
ln Vivo |
Icerguastat (4–8 mg/kg; intraperitoneally; daily for 35 days) postpones the body's reaction to experimental autoimmune encephalitis (EAE). Infection is prolonged once with iceraguastat (100 μg; ip). Premon
|
Animal Protocol |
Animal/Disease Models: C57BL/6J female mice were immunized with MOG35-55/CFA to induce chronic EAE[1]
Doses: 4 mg/kg, 8 mg/kg Route of Administration: Ip ;The lifetime of the virus in mice [3]. one time/day for 35 days Experimental Results: Both doses Dramatically delayed the onset of clinical disease, but the delay was greater with the 8 mg/kg treatment. Animal/Disease Models: Fiveweeks old female FVB mice (intracerebral injection of mouse-adapted RML prions) [3] Doses: 100 μg Route of Administration: intraperitoneal (ip) injection; 3 times a week for 60 days, treatment after 60 days Reduce to twice weekly intraperitoneal (ip) injections for 20 days. Experimental Results: Dramatically prolonged survival of prion-infected mice. |
References |
|
Molecular Formula |
C8H9N4CL
|
---|---|
Molecular Weight |
196.637
|
Exact Mass |
196.051
|
Elemental Analysis |
C, 48.87; H, 4.61; Cl, 18.03; N, 28.49
|
CAS # |
951441-04-6
|
Related CAS # |
(E/Z)-Icerguastat;13098-73-2
|
PubChem CID |
9561611
|
Appearance |
White to off-white solid powder
|
Density |
1.4±0.1 g/cm3
|
Boiling Point |
374.2±44.0 °C at 760 mmHg
|
Flash Point |
180.1±28.4 °C
|
Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
Index of Refraction |
1.626
|
LogP |
1.79
|
Hydrogen Bond Donor Count |
2
|
Hydrogen Bond Acceptor Count |
2
|
Rotatable Bond Count |
2
|
Heavy Atom Count |
13
|
Complexity |
210
|
Defined Atom Stereocenter Count |
0
|
SMILES |
C(/C1C=CC=CC=1Cl)=N\NC(N)=N
|
InChi Key |
PDWJALXSRRSUHR-LFYBBSHMSA-N
|
InChi Code |
InChI=1S/C8H9ClN4/c9-7-4-2-1-3-6(7)5-12-13-8(10)11/h1-5H,(H4,10,11,13)/b12-5+
|
Chemical Name |
2-[(E)-(2-chlorophenyl)methylideneamino]guanidine
|
Synonyms |
Sephin1; Sephin-1; Sephin 1, icerguastatum; icerguastat
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~50 mg/mL (~254.27 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (10.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 5.0854 mL | 25.4272 mL | 50.8544 mL | |
5 mM | 1.0171 mL | 5.0854 mL | 10.1709 mL | |
10 mM | 0.5085 mL | 2.5427 mL | 5.0854 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.