Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Purity: = 100%
SB-334867 is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with a pKb value of 7.2. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been demonstrated to have sedative and anorectic effects in animals. It has also proven helpful in defining how orexinergic regulation of brain systems related to appetite, sleep, and other physiological processes is regulated.
Targets |
OX1 receptor
|
||
---|---|---|---|
ln Vitro |
|
||
ln Vivo |
|
||
Enzyme Assay |
SB-334867 free base has an IC50 value of 7.2 (pKb) and is a selective non-peptide orexin OX1 receptor antagonist. In CHO-OX(1) cells, SB-334867-A did not affect the calcium response induced by UTP (3 microM) but it did suppress the responses to orexin-A (10 nM) and orexin-B (100 nM) (pK(B)=7.27+/-0.04 and 7.23+/-0.03, respectively, n=8). The calcium responses mediated by OX(2) were also inhibited by SB-334867-A (10 microM) (32.7+/-1.9% versus orexin-A).
|
||
Cell Assay |
Two peptides extracted from the rat hypothalamus are called orexin-A and orexin-B. Some physiological processes that they are involved in include feeding regulation, energy metabolism, and sleep-wake cycle regulation. In CHO-OX1 cells, SB-334867 can suppress the calcium responses induced by orexin-A and orexin-B, with pKB values of 7.27 and 7.23, respectively. For OX1 receptors, SB-334867 exhibits greater selectivity than OX2 receptors. It inhibits the calcium responses in CHO-OX2 cells that are induced by orexin-A by 32.7% and orexin-B by 22%, respectively.
|
||
Animal Protocol |
|
||
References |
|
Molecular Formula |
C17H13N5O2
|
|
---|---|---|
Molecular Weight |
319.32
|
|
Exact Mass |
319.11
|
|
Elemental Analysis |
C, 63.94; H, 4.10; N, 21.93; O, 10.02
|
|
CAS # |
792173-99-0
|
|
Related CAS # |
SB-334867; 249889-64-3
|
|
Appearance |
Solid powder
|
|
SMILES |
CC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4
|
|
InChi Key |
AKMNUCBQGHFICM-UHFFFAOYSA-N
|
|
InChi Code |
InChI=1S/C17H13N5O2/c1-10-20-12-5-4-11(9-15(12)24-10)21-17(23)22-14-6-8-18-13-3-2-7-19-16(13)14/h2-9H,1H3,(H2,18,21,22,23)
|
|
Chemical Name |
1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
|
|
Synonyms |
|
|
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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 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 25.0 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: 2.5 mg/mL (7.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% CMC Na : 30mg/mL Solubility in Formulation 5: 10 mg/mL (31.32 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 7.69 mg/mL (24.08 mM) in 50% HP-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1317 mL | 15.6583 mL | 31.3165 mL | |
5 mM | 0.6263 mL | 3.1317 mL | 6.2633 mL | |
10 mM | 0.3132 mL | 1.5658 mL | 3.1317 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.