TG100-115
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1045 | Check With Us |
| 500mg | $1672 | Check With Us |
| 1g | $2508 | Check With Us |
: Cat #: V0129 CAS #: 677297-51-7 Purity ≥ 98%
Description: TG100-115 is a novel, potent and selective PI3Kγ/δ inhibitor with potential cardioprotecting effects.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 346.34 |
|---|---|
| Molecular Formula | C18H14N6O2 |
| CAS No. | 677297-51-7 |
| Storage | -20℃ for 3 years in powder form; r |
| -80℃ for 2 years in solven | |
| Solubility In Vitro | DMSO: 9 mg/mL (25.98 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: <1 mg/m | |
| Solubility In Vivo | 5% DMSO+30% PEG 300+ddH2O: 0.4mg/mL |
| SMILES Code | OC1=CC=CC(C2=NC3=NC(N)=NC(N)=C3N=C2C4=CC=CC(O)=C4)=C1 |
| Synonyms | TG100115; TG-100115; TG 100115; TG-100-115; TG100-115 ; TG 100-115 |
| Protocol | In Vitro | TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50 values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50 values <1 μM. TG100-115 potently inhibits edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage. |
|---|---|---|
| In Vivo | To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.8873 mL | 14.4367 mL | 28.8734 mL | 57.7467 mL |
| 5mM | 0.5775 mL | 2.8873 mL | 5.7747 mL | 11.5493 mL |
| 10mM | 0.2887 mL | 1.4437 mL | 2.8873 mL | 5.7747 mL |
| 20mM | 0.1444 mL | 0.7218 mL | 1.4437 mL | 2.8873 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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,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 master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.