| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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Purity: ≥98%
LY2794193 is a novel, highly potent and selective mGlu3 receptor agonist with Ki / EC50 of 0.927 nM / 0.47 nM; 412 nM / 47.5 nM for hmGlu3 and hmGlu2, respectively.
| ln Vitro |
In cultured paired cortical neurons, LY2794193 suppresses spontaneous Ca2+ oscillations with an EC50 of 43.6 nM[1]. With a combined maximal agonist efficacy (Emax) of 66%, LY2794193 demonstrates biphasic suppression of spontaneous Ca2+ transients in a coupled neuronal Ca2+ oscillation experiment (high affinity, EC50=0.44 nM; 48% of total agonist response; low affinity, EC50=43.6 nM; 52% of total agonist response) [1].
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| ln Vivo |
A dose-related decrease in walking is brought on by LY2794193 (1–30 mg/kg, subcutaneous injection), which is administered 30 minutes prior to PCP (5 mg/kg, subcutaneous injection) [1]. In cotton Sprague-Dawley, LY2794193 (1 mg/kg; iv) has an estimated half-life (T1/2) of 3.1 h, intermediate clearance (18.3 mL/min/kg), and SE (1.17 L/kg) [1]. LY2794193 (3 mg/kg; sc) produced an estimated bioavailability of 121% in the Sprague-Dawley, resulting in a quick shelf appearance (AUC=9.9 μM; Cmax=6.78 μM; Tmax=0.44 h) [1].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats
Doses: 1, 3, 10, or 30 mg/kg Route of Administration: subcutaneously (sc) (sc); subcutaneously (sc) (sc); 30 minutes before PCP (5 mg/kg, subcutaneously (sc) (sc)) Experimental Results: Observed and Dose There was an associated reduction in activity that was statistically significant at the 10 and 30 mg/kg doses. |
| References |
| Molecular Formula |
C16H18N2O6
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|---|---|
| Molecular Weight |
334.323924541473
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| Exact Mass |
334.116
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| CAS # |
2173037-97-1
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| PubChem CID |
60096231
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| Appearance |
White to off-white solid powder
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| LogP |
-2.6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
567
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| Defined Atom Stereocenter Count |
5
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| SMILES |
OC([C@H]1[C@@H]2[C@H](C[C@@](C(=O)O)([C@@H]21)N)NC(C1C=CC=C(C=1)OC)=O)=O
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| InChi Key |
UXNRHIJPZNNDDJ-VZAVHYRXSA-N
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| InChi Code |
InChI=1S/C16H18N2O6/c1-24-8-4-2-3-7(5-8)13(19)18-9-6-16(17,15(22)23)12-10(9)11(12)14(20)21/h2-5,9-12H,6,17H2,1H3,(H,18,19)(H,20,21)(H,22,23)/t9-,10-,11-,12-,16-/m0/s1
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| Chemical Name |
(1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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| Synonyms |
LY2794193; LY-2794193; LY 2794193
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~598.23 mM)
H2O : ~2 mg/mL (~5.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 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. Solubility in Formulation 2: ≥ 5 mg/mL (14.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9911 mL | 14.9557 mL | 29.9115 mL | |
| 5 mM | 0.5982 mL | 2.9911 mL | 5.9823 mL | |
| 10 mM | 0.2991 mL | 1.4956 mL | 2.9911 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.
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