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CB7921220

Cat No.:V17663 Purity: ≥98%
CB-7921220 is an inhibitor (blocker/antagonist) of adenylate cyclase.
CB7921220
CB7921220 Chemical Structure CAS No.: 115453-99-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
Other Sizes
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Product Description
CB-7921220 is an inhibitor (blocker/antagonist) of adenylate cyclase.
CB7921220 (CB-7921220) is an inhibitor of adenylyl cyclase (AC). It shows a degree of isoform selectivity for adenylyl cyclase 1 (AC1), but cannot distinguish between AC1 and AC6. It is a small molecule with the IUPAC name 6-[(E)-2-(4-aminophenyl)ethenyl]pyridine-2-carboxylic acid. CB7921220 is used in research to study cAMP signaling pathways.
Biological Activity I Assay Protocols (From Reference)
Targets
CB7921220 targets adenylyl cyclase (AC) isoforms AC1 and AC6. Adenylyl cyclase is an enzyme that converts ATP to cyclic AMP (cAMP), an important second messenger in many biological processes. By inhibiting AC1 and AC6, CB7921220 reduces cAMP production and modulates downstream signaling pathways. It shows no effect on AC2 and AC5.
ln Vitro
Adenylyl cyclase (AC) 1 has some isoform selectivity in CB-7921220, yet it is unable to distinguish between AC1 and AC6. The lack of selectivity of CB-7921220 between AC1 and AC6 may be explained by its more consistently predicted binding position in the two virtual docking screens and similar binding conformation to ATP and P-site inhibitors [1].
CB7921220 is a selective inhibitor of adenylyl cyclase isoforms AC1 and AC6. At a concentration of 100 μM, it reduces AC1 and AC6 activity by 60% in Sf9 membranes stimulated by forskolin. It has no effect on AC2 and AC5, demonstrating isoform selectivity.
ln Vivo
Specific in vivo activity data for CB7921220 is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of AC1 and AC6 inhibition and its impact on cAMP-mediated signaling pathways. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties.
Enzyme Assay
CB7921220's activity as an AC inhibitor is assessed using in vitro enzyme assays that measure its ability to inhibit adenylyl cyclase activity. These assays typically involve measuring cAMP production in cell membranes or purified enzyme preparations. The compound's selectivity for AC1 and AC6 over AC2 and AC5 is evaluated.
Cell Assay
Cellular assays for CB7921220 involve treating cells with the compound and measuring cAMP levels and downstream signaling. The compound's ability to inhibit AC1 and AC6-mediated cAMP production is assessed. Its effects on cellular processes regulated by cAMP, such as gene expression and cell function, are evaluated.
Animal Protocol
In vivo animal model protocols for CB7921220 would involve its administration to animal models to study the role of AC1 and AC6 in various physiological and pathological processes. The compound's effects on cAMP signaling, behavior, and disease phenotypes would be assessed.
ADME/Pharmacokinetics
CB7921220 has a molecular weight of 240.26 and a molecular formula of C14H12N2O2. It is supplied as a powder or in solution. Specific pharmacokinetic data is not extensively detailed in the available literature. As a small molecule inhibitor, its pharmacokinetic properties would need to be evaluated in preclinical studies.
Toxicity/Toxicokinetics
CB7921220 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. Standard safety assessments would be required for clinical development.
References

[1]. Isoform selectivity of adenylyl cyclase inhibitors: characterization of known and novel compounds. J Pharmacol Exp Ther. 2013 Nov;347(2):265-75.

Additional Infomation
CB7921220 (CAS# 115453-99-1) is a research compound used to study adenylyl cyclase function and cAMP signaling. It is a selective inhibitor of AC1 and AC6. It is not approved for clinical use and is supplied as a research chemical.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H12N2O2
Molecular Weight
240.257283210754
Exact Mass
240.09
CAS #
115453-99-1
PubChem CID
5740547
Appearance
Pink to red solid powder
Melting Point
225 - 226 °C
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
3
Heavy Atom Count
18
Complexity
309
Defined Atom Stereocenter Count
0
SMILES
C1=CC(=NC(=C1)C(=O)O)/C=C/C2=CC=C(C=C2)N
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 Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~208.11 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.1622 mL 20.8108 mL 41.6216 mL
5 mM 0.8324 mL 4.1622 mL 8.3243 mL
10 mM 0.4162 mL 2.0811 mL 4.1622 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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