| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
p5-HT1 (Ki=1.2 μM), p5-HT2 (Ki=0.52 μM), and pα1 (Ki=0.27 μM) are all inhibited by FAUC 213[1].
|
|---|---|
| ln Vivo |
Even at just 30 mg/kg before treatment, FAUC 213 (7.5–30 mg/kg; oral; single dosage) dramatically decreased AMPH-induced elevations in hyperkinesia. The reduction in prepulse inhibition (PPI) caused by apomorphine (APO) administration at a dose of 30 mg/kg was dramatically recovered by FAUC 213 [1].
|
| Animal Protocol |
Animal/Disease Models: Male adult Wistar rats, body weight 300-350 g[1]
Doses: 7.5, 15, 30 mg/kg Route of Administration: oral; single dose Experimental Results: pretreatment with only 30 mg/kg can Dramatically Reduces the increase in amphetamine (AMPH)-induced hyperkinesia. |
| References |
[1]. Frank Boeckler, et al. FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Psychopharmacology (Berl). 2004 Aug;175(1):7-17.
|
| Molecular Formula |
C18H19CLN4
|
|---|---|
| Molecular Weight |
326.82
|
| Exact Mass |
326.13
|
| CAS # |
337972-47-1
|
| PubChem CID |
10336538
|
| Appearance |
White to off-white solid powder
|
| Density |
1.28g/cm3
|
| Index of Refraction |
1.667
|
| LogP |
3.312
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
377
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC2=CC(=NN2C=C1)CN3CCN(CC3)C4=CC=C(C=C4)Cl
|
| InChi Key |
DTRXURJDKOYCCD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H19ClN4/c19-15-4-6-17(7-5-15)22-11-9-21(10-12-22)14-16-13-18-3-1-2-8-23(18)20-16/h1-8,13H,9-12,14H2
|
| Chemical Name |
2-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]pyrazolo[1,5-a]pyridine
|
| Synonyms |
FAUC213; FAUC 213; FAUC-213
|
| 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) |
DMSO : ~100 mg/mL (~305.98 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (3.82 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 12.5 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0598 mL | 15.2989 mL | 30.5979 mL | |
| 5 mM | 0.6120 mL | 3.0598 mL | 6.1196 mL | |
| 10 mM | 0.3060 mL | 1.5299 mL | 3.0598 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
