GNE-7915 tosylate
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $489 | Check With Us |
500mg | $739 | Check With Us |
1g | $1105 | Check With Us |
Cat #: V3835 CAS #: 2070015-00-6 Purity ≥ 98%
Description: GNE-7915 tosylate is a novel, highly potent, selective, and brain-penetrant leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively.
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Molecular Weight (MW) | 615.60 |
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Molecular Formula | C₂₆H₂₉F₄N₅O₆S |
CAS No. | 2070015-00-6 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 22 mg/mL (49.6 mM)r |
Water: <1 mg/mLr | |
Ethanol: <1 mg/mL | |
SMILES Code | CCNC1=NC(NC2=C(OC)C=C(C(N3CCOCC3)=O)C(F)=C2)=NC=C1C(F)(F)F.CC4=CC=C(S(=O)(O)=O)C=C4 |
Synonyms | GNE7915 tosylate; GNE 7915 tosylate; GNE-7915 tosylate |
Protocol | In Vitro | Maintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 μM for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE-7915 at 0.1 μM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitro functional assays. |
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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 | 1.6244 mL | 8.1222 mL | 16.2443 mL | 32.4886 mL |
5mM | 0.3249 mL | 1.6244 mL | 3.2489 mL | 6.4977 mL |
10mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 3.2489 mL |
20mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 1.6244 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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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
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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.