Valrocemide, formerly known as TV-1901, is an antiepileptic drug (AED). Valrocemide has a broad spectrum of anticonvulsant activity and promising potential as a new AED. Valrocemide is an anticonvulsant agent under development by Teva and Acorda as a potential therapeutic for the treatment of epilepsy.

Physicochemical Properties

Molecular Formula	C10H20N2O2
Molecular Weight	200.282
Exact Mass	200.152
CAS #	92262-58-3
Related CAS #	92262-58-3
PubChem CID	6918293
Appearance	White to off-white solid powder
Density	0.997
Boiling Point	417.5ºC at 760 mmHg
Flash Point	206.3ºC
Index of Refraction	1.465
LogP	1.895
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	7
Heavy Atom Count	14
Complexity	187
Defined Atom Stereocenter Count	0
SMILES	O=C(CNC(C(CCC)CCC)=O)N
InChi Key	RALGCAOVRLYSMA-UHFFFAOYSA-N
InChi Code	InChI=1S/C10H20N2O2/c1-3-5-8(6-4-2)10(14)12-7-9(11)13/h8H,3-7H2,1-2H3,(H2,11,13)(H,12,14)
Chemical Name	N-(2-amino-2-oxoethyl)-2-propylpentanamide
Synonyms	Valrocemide TV-1901 TV 1901 TV1901 SPD-493 TVP-1901 SPD493 TVP1901 SPD 493 TVP 1901. N-Valproyl glycinamide.
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
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vivo	The study found that mice were completely protected against 6 Hz "psychomotor" seizures as well as seizures caused by pentylenetetrazole, picrotoxin, and bicuculline, with median effective dosage (ED50) values of 151, 132, 275, 248, and 237 mg/kg, respectively. In Frings audiogenic epilepsy-susceptible mice, valrocemide likewise effectively prevents sound-induced seizures (ED50, 52 mg/kg). 332 mg/kg was the median hazardous dosage in mice. Vasotecime was active in the MES test after oral administration to rats, with an ED50 of 73 mg/kg and a median neurotoxic dosage of 1,000 mg/kg. In Sprague-Dawley rats with hippocampally ignited hippocampus, an intraperitoneal dose of 300 mg/kg prolosemide avoided generalized seizures and markedly reduced the afterdischarge period. Rats with corneal ignition were similarly completely protected against focal seizures (ED50, 161 mg/kg) by valrocemide [1].
References	[1]. Isoherranen N, et al. Anticonvulsant profile of valrocemide (TV1901): a new antiepileptic drug. Epilepsia. 2001 Jul;42(7):831-6
Additional Infomation	Drug Indication Investigated for use/treatment in epilepsy.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~499.30 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.75 mg/mL (13.73 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 27.5 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: ≥ 2.75 mg/mL (13.73 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 27.5 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 3: ≥ 2.75 mg/mL (13.73 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 27.5 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	4.9930 mL	24.9650 mL	49.9301 mL
	5 mM	0.9986 mL	4.9930 mL	9.9860 mL
	10 mM	0.4993 mL	2.4965 mL	4.9930 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.