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Purity: ≥98%
SB-222200 is a novel, potent, selective, reversible, brain penetrant and competitive antagonist of human NK-3 receptor with Ki of 4.4 nM. SB-222200 counteracted NKB-induced Ca(2+) mobilization in HEK 293 cells that were stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM.It also inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM. Comparing hNK-3 receptors to hNK-1 (K(i) > 100,000 nM) and hNK-2 (K(i) = 250 nM) receptors, SB-222200 was more selective for your target.
| Targets |
NK3
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|---|---|
| ln Vitro |
SB-222200 prevents CHO cell membranes from being bound by 125I-[MePhe7]neurokinin B (NKB), which is necessary for the stable expression of the hNK-3 receptor (CHO-hNK-3R) at a Ki of 4.4 nM[1].
SB-222200 stably expresses the hNK-3 receptor (HEK 293-hNK-3R), inhibiting NKB-induced Ca2+ mobilization in these cells with an IC50 of 18.4 nM[1]. SB-222200 is hNK-3 receptor selective as opposed to hNK-1 (Ki>100,000 nM) and hNK-2 (Ki=250 nM) receptors[1]. SB-222200 (10 nM-1 μM) inhibits NKB-induced Ca2+ mobilization in a concentration-dependent and surmountable manner in HEK 293-hNK-3R cells[1]. |
| ln Vivo |
SB-222200 (5 mg/kg; 30 min pretreatment) produces inhibition of behavioral responses in mice induced by senktide (HY-P0187), a selective agonist of the NK-3 receptor[1].
SB-2222006 indicates that after oral administration of 10 mg/kg, the rat has a moderate oral bioavailability (46%) and a Cmax of 427 ng/mL[1]. SB-2222006 displays a terminal elimination half-life of 1.9 hours in rats as a result of a high plasma clearance of 56 mL/min/kg after intravenous administration of 2.5 mg/kg.[1]. |
| Animal Protocol |
Male BALB/c mice (19-21 g)
5 mg/kg Oral administration |
| References |
| Molecular Formula |
C26H24N2O
|
|---|---|
| Molecular Weight |
380.4816
|
| Exact Mass |
380.19
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| Elemental Analysis |
C, 82.07; H, 6.36; N, 7.36; O, 4.20
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| CAS # |
174635-69-9
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| Appearance |
Solid powder
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| SMILES |
3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide
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| InChi Key |
MQNYRKWJSMQECI-QFIPXVFZSA-N
|
| InChi Code |
InChI=1S/C26H24N2O/c1-3-22(19-12-6-4-7-13-19)28-26(29)24-18(2)25(20-14-8-5-9-15-20)27-23-17-11-10-16-21(23)24/h4-17,22H,3H2,1-2H3,(H,28,29)/t22-/m0/s1
|
| Chemical Name |
3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide
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| Synonyms |
SB222200; SB-222200; SB 222200
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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: ≥ 100 mg/mL (~262.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 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 (6.57 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 25.0 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 | 2.6283 mL | 13.1413 mL | 26.2826 mL | |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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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