| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
AC1 ( IC50 = 2.3 μM )
ST034307 is a potent and selective inhibitor of adenylyl cyclase 1 (AC1), a key enzyme involved in the production of cyclic adenosine monophosphate (cAMP). The compound exhibits an IC50 of 2.3 μM for AC1 inhibition and shows selectivity over other AC isoforms. AC1 has been identified as a potential target for treating pain and reducing opioid dependence, as it plays a role in pain signaling pathways. By selectively inhibiting AC1, ST034307 modulates cAMP production and downstream signaling pathways involved in neurotransmission and pain perception. It slightly increases the activity of AC8, indicating isoform selectivity. |
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| ln Vitro |
ST034307 shows that AC1 is selectively inhibited, and it slightly increases the activity of AC8. Phenol-12-myristate 13-acetate (PMA)-stimulated cAMP production by AC2 is enhanced by ST034307. Forskolin- or isoproterenol-stimulated AC1 activity in HEK cells that express AC1 is markedly inhibited by ST034307. In contrast, ST034307 has no discernible effects on HEK cells that are wild-type. The accumulation of cAMP in the hippocampal homogenates stimulated by Ca2+ and calmodulin is strongly inhibited by ST034307. In a dose-dependent manner, ST034307 prevents AC1's MOR-mediated sensitization from developing and from continuing[1].
In vitro, ST034307 significantly inhibits forskolin- or isoproterenol-stimulated AC1 activity in HEK cells stably expressing AC1. The compound reduces Ca2+/calmodulin-stimulated cAMP accumulation in hippocampal homogenates. It exhibits an IC50 of 2.3 μM for AC1 inhibition. The compound does not show significant activity against AC8, indicating selectivity for the AC1 isoform. These in vitro studies demonstrate that ST034307 effectively inhibits AC1 enzymatic activity and reduces cAMP production in cellular and tissue homogenate models. |
| ln Vivo |
ST034307 (0.25 μg) significantly reduces inflammatory pain induced by CFA in mice. ST034307 has an estimated median effective dose (E50) value of 0.28 μg for analgesia in the mouse pain model[1].
In vivo, ST034307 has shown analgesic activity in preclinical models. As a selective inhibitor of adenylyl cyclase 1 (AC1), it modulates cAMP signaling pathways involved in pain perception. AC1 has been shown to be a potential target for treating pain and reducing opioid dependence. The compound's ability to modulate adenylyl cyclase activity may have implications in various signaling pathways mediated by cAMP, such as those involved in neurotransmission and cellular responses to hormones and neurotransmitters. ST034307 is being investigated for its potential therapeutic applications in pain management. |
| Enzyme Assay |
In vitro enzyme assays for ST034307 involve measuring the inhibition of adenylyl cyclase 1 (AC1) enzymatic activity. The compound is tested against purified AC1 enzyme or in cell-based systems stably expressing AC1. The inhibition is quantified by determining the IC50, which is 2.3 μM. The assay typically measures the production of cyclic AMP (cAMP) in response to forskolin or isoproterenol stimulation. The compound's selectivity is assessed by testing its activity against other AC isoforms, such as AC8. These enzyme assays confirm the mechanism of action as a selective AC1 inhibitor.
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| Cell Assay |
HEK-AC1 cells are used in cell viability assays, and the plating and compound incubation protocols used are the same as those outlined in "cAMP accumulation in cells." Cell viability is expressed as a percentage of vehicle, with a control of 2% Triton X-100. As directed by the manufacturer, cell viability is evaluated using the Promega CellTiter-Glo Luminescent Cell Viability Assay kit. Synergy 4 is used to measure luminosity counts.
In vitro cellular assays for ST034307 typically involve HEK cells stably expressing AC1. Cells are treated with the compound and stimulated with forskolin or isoproterenol to activate AC1. The inhibition of AC1 activity is measured by quantifying the production of cyclic AMP (cAMP) using standard assays such as ELISA or radioimmunoassay. The compound exhibits an IC50 of 2.3 μM for AC1 inhibition in these cellular systems. These cell-based assays confirm that ST034307 effectively inhibits AC1 activity in a cellular context and demonstrates selectivity over other AC isoforms. |
| Animal Protocol |
In vivo animal models for ST034307 typically involve pain models such as the formalin test, hot plate test, or tail flick test in rodents. The compound is administered by appropriate routes (e.g., oral or intraperitoneal), and its analgesic efficacy is assessed by measuring the reduction in pain responses. Doses are optimized based on the specific model and experimental objectives. AC1 has been identified as a potential target for pain management, and ST034307's ability to inhibit AC1 makes it a candidate for these studies. These animal studies provide evidence for the compound's in vivo analgesic activity.
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| ADME/Pharmacokinetics |
ST034307 is a small-molecule inhibitor of adenylyl cyclase 1 (AC1) with a molecular weight of 297.9 g/mol. It is soluble in DMSO (up to 100 mM) and ethanol (up to 20 mM). The compound is typically stored at -20°C. Its chemical structure is 6-Chloro-2-(trichloromethyl)-4H-1-benzopyran-4-one. ST034307 is designed to selectively inhibit AC1 without affecting other AC isoforms vital to physiological functions, which has been a challenge in drug development. The compound's favorable solubility properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
ST034307 is a selective inhibitor of adenylyl cyclase 1 (AC1) with an IC50 of 2.3 μM. It has been investigated for its potential therapeutic applications in pain management and reducing opioid dependence. The compound's selectivity for AC1 over other AC isoforms is a key feature, as it minimizes off-target effects. ST034307 is for research use only and is not approved for human therapeutic use. It represents a promising tool compound for studying the role of AC1 in pain signaling and other cAMP-mediated pathways.
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| References |
| Molecular Formula |
C10H4CL4O2
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|---|---|
| Molecular Weight |
297.949559211731
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| Exact Mass |
295.897
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| Elemental Analysis |
C, 40.31; H, 1.35; Cl, 47.59; O, 10.74
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| CAS # |
133406-29-8
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| Related CAS # |
133406-29-8
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| PubChem CID |
867466
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.273
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
16
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C(Cl)(Cl)Cl)OC2=CC=C(Cl)C=C2C(=O)C=1
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| InChi Key |
NTDHYMSVCBGQJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H4Cl4O2/c11-5-1-2-8-6(3-5)7(15)4-9(16-8)10(12,13)14/h1-4H
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| Chemical Name |
6-chloro-2-(trichloromethyl)chromen-4-one
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| Synonyms |
ST034307
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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: ~16 mg/mL (~53.7 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.60 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 16.7 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: ≥ 1.67 mg/mL (5.60 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 16.7 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 | 3.3563 mL | 16.7813 mL | 33.5627 mL | |
| 5 mM | 0.6713 mL | 3.3563 mL | 6.7125 mL | |
| 10 mM | 0.3356 mL | 1.6781 mL | 3.3563 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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