| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SRX-246 targets the vasopressin 1a (V1a) receptor, a G protein-coupled receptor that mediates the effects of the neuropeptide arginine vasopressin (AVP). As a potent, selective, and CNS-penetrant antagonist, SRX-246 blocks V1a receptor signaling in the brain. It has a Ki of 0.3 nM for the human V1a receptor.
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| ln Vitro |
SRX-246 is a potent and highly selective vasopressin 1a (V1a) receptor antagonist with a Ki of 0.3 nM for the human V1a receptor. It has no interaction at V1b and V2 receptors, demonstrating excellent selectivity. The compound is CNS-penetrating and orally bioavailable.
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| ln Vivo |
The Cmax, AUC0-∞, and t1/2 values for SRX246 (2 mg/kg; iv) therapy were 953 ng/mL and 1141 ng, respectively.For post-pharmacokinetics, the values are h/mL and 6.02 hours, respectively. (dosage 20 mg/kg), 98.4 ng/mL, 624 ng, and AUC0-∞ are the Cmax, AUC0-∞, and t1/2 values.m/mL and 2.38 hours, in that order [1].
SRX-246 is orally bioavailable and CNS-penetrating, making it suitable for in vivo studies of V1a receptor function in the brain. As a V1a receptor antagonist, it has potential for the treatment of conditions involving vasopressin signaling dysregulation, such as aggression, anxiety, and social behavior disorders. |
| Enzyme Assay |
The binding affinity of SRX-246 to the V1a receptor can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human V1a receptors. Competition binding experiments are performed with increasing concentrations of SRX-246 against a fixed concentration of a radiolabeled V1a receptor ligand. Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of SRX-246 at the V1a receptor is evaluated in vitro using cells expressing recombinant V1a receptors. Cells are treated with increasing concentrations of SRX-246, and V1a receptor-mediated signaling, such as intracellular calcium mobilization, is measured. The ability of SRX-246 to antagonize AVP-induced signaling is assessed.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [1].
Doses: 2 mg/kg (oral 20 mg/kg) Route of Administration: iv (pharmacokinetic/PK/PK analysis) Experimental Results: After iv administration, the plasma concentration diminished steadily, with a half-life (t1/2) of 6 hrs (hrs (hours)). The Cmax and AUC0-∞ values were 953 ng/mL, 1141 ng·h/mL, 6.02 hrs (hrs (hours)). After oral administration, the Cmax, AUC0-∞ and t1/2 values were 98.4 ng/mL, 624 ng·h/mL and 2.38 hrs (hrs (hours)) respectively. SRX-246 is administered orally to animal models for evaluating its in vivo effects on V1a receptor-mediated behaviors. In rodent models, SRX-246 is given at various doses via oral gavage. Behavioral tests related to aggression, anxiety, social interaction, and stress responses are performed to assess V1a receptor blockade. |
| ADME/Pharmacokinetics |
SRX-246 has a molecular formula of C42H49N5O5 and a molecular weight of 703.87. It is orally bioavailable and CNS-penetrating. In solvent, it can be stored at -20°C for 3-6 months or at -80°C for 12 months. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of SRX-246 is not extensively documented. As a V1a receptor antagonist, potential adverse effects may include those related to vasopressin receptor blockade, such as effects on water homeostasis and cardiovascular function. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
SRX-246 (CAS# 512784-93-9) is a potent, CNS-penetrating, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist with a Ki of 0.3 nM for the human V1a receptor. It has no interaction at V1b and V2 receptors. SRX-246 is a research tool for studying vasopressin signaling in the brain.
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| Molecular Formula |
C42H49N5O5
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|---|---|
| Molecular Weight |
703.868970632553
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| Exact Mass |
703.373
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| CAS # |
512784-93-9
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| PubChem CID |
44428550
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| Appearance |
White to off-white solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
52
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| Complexity |
1260
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1C(N([C@@H](C2C=CC=CC=2)C1)[C@@H]1C(N([C@@H](C(N[C@H](C)C2C=CC=CC=2)=O)CC(N2CCC(CC2)N2CCCCC2)=O)[C@@H]1/C=C/C1C=CC=CC=1)=O)=O
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| InChi Key |
FJUKOXWSIGULLE-JVOQCOEYSA-N
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| InChi Code |
InChI=1S/C42H49N5O5/c1-30(32-16-8-3-9-17-32)43-40(49)36(28-38(48)45-26-22-34(23-27-45)44-24-12-5-13-25-44)46-35(21-20-31-14-6-2-7-15-31)39(41(46)50)47-37(29-52-42(47)51)33-18-10-4-11-19-33/h2-4,6-11,14-21,30,34-37,39H,5,12-13,22-29H2,1H3,(H,43,49)/b21-20+/t30-,35-,36-,37-,39+/m1/s1
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| Chemical Name |
(2R)-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-N-[(1R)-1-phenylethyl]-4-(4-piperidin-1-ylpiperidin-1-yl)butanamide
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| Synonyms |
SRX 246; SRX246; SRX-246
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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 (~142.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.55 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 (3.55 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 | 1.4207 mL | 7.1036 mL | 14.2072 mL | |
| 5 mM | 0.2841 mL | 1.4207 mL | 2.8414 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4207 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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