| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
NMDA Receptor
|
|---|---|
| ln Vitro |
Internal methylation of viral RNA in B77 transformed chick embryo fibroblasts is blocked by cycloleucine (4–40 mM; 3 h)[5]. More than 90% of B77 38S RNA subunits are prevented from forming the penultimate Gm and m6A by cycloleucine (40 mM; 24 h)[5]. ?The viability of human KB and mouse L1210s leukemia cell lines is inhibited by cytostatic (10 μg/mL)[5].
|
| ln Vivo |
In rats, cycloleucine (0.5–4 μg; intracerebroventricular injection) prolongs open arm entry, increases open arm duration, and causes severe arrivals[3]. In mice infected with the Semliki Forest virus (SFV) strain A7(74) and normal mice, cycloleucine lowers the weights of the spleen and thymus[6].
|
| Animal Protocol |
Animal/Disease Models: Male rats bilaterally cannulated into the nucleus accumbens septi (NAS)[3]
Doses: 1 µL of 0.5, 1.0, 2.0, 4 µg/µL Route of Administration: Intracerebroventrical injection Experimental Results: Increased time spent in the open arms and extreme arrivals at all doses. Increased open arm entries at the dose of 4 μg. |
| References |
[1]. Hood WF, et, al. 1-Aminocyclobutane-1-carboxylate (ACBC): a specific antagonist of the N-methyl-D-aspartate receptor coupled glycine receptor. Eur J Pharmacol. 1989 Feb 28;161(2-3):281-2.
[2]. Caboche M, et, al. RNA methylation and control of eukaryotic RNA biosynthesis. Effects of cycloleucine, a specific inhibitor of methylation, on ribosomal RNA maturation. Eur J Biochem. 1977 Mar 15;74(1):19-29. [3]. Gargiulo API, et, al. Effects of Cycloleucine in the Nucleus Accumbens Septi on the Elevated plus Maze Test in Rats. Neuropsychobiology. 2020;79(3):191-197. [4]. Duś D, et, al. Cytostatic activity in vitro of cycloleucine, aspartic acid and glutamic acid phosphonic analogues. Arch Immunol Ther Exp (Warsz). 1980;28(3):433-8. [5]. Dimock K, et, al. Cycloleucine blocks 5'-terminal and internal methylations of avian sarcoma virus genome RNA. Biochemistry. 1978 Aug 22;17(17):3627-32. [6]. S Amor, et al. The effect of cycloleucine on SFV A7(74) infection in mice. Br J Exp Pathol. 1987 Apr;68(2):225-35. |
| Molecular Formula |
C6H11NO2
|
|---|---|
| Molecular Weight |
129.16
|
| CAS # |
52-52-8
|
| SMILES |
O=C(C1(CCCC1)N)O
|
| 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)
|
| Solubility (In Vitro) |
H2O: 20 mg/mL (154.85 mM)
DMSO: < 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (774.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.7423 mL | 38.7117 mL | 77.4234 mL | |
| 5 mM | 1.5485 mL | 7.7423 mL | 15.4847 mL | |
| 10 mM | 0.7742 mL | 3.8712 mL | 7.7423 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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