2. Immunology/Inflammation MAPK/ERK Pathway TGF-beta/Smad Stem Cell/Wnt Neuronal Signaling Membrane Transporter/Ion Channel
  3. PKA Cyclic GMP-AMP Synthase ERK Calcium Channel
  4. HA-1004

HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.

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HA-1004 Chemical Structure

HA-1004 Chemical Structure

CAS No. : 91742-10-8

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of HA-1004:

HA-1004 Related Antibodies

Top Publications Citing Use of Products

View All PKA Isoform Specific Products:

View All Isoforms
PKA PKAR

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All Calcium Channel Isoform Specific Products:

View All Isoforms
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models[1][2][3].

IC50 & Target

cyclic GMP-dependent protein kinase, cyclic AMP-dependent protein[2]
In Vivo

HA-1004 (40 nmol/day; infused by minipumps and delivered at 1 μL/h), it acts simultaneously with morphine to antagonize the phosphorylation of ERK1/2 and TH and inhibit the increase of NA conversion during morphine withdrawal in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

293.34

Formula

C12H15N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC(N)=N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (170.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4090 mL 17.0451 mL 34.0901 mL
5 mM 0.6818 mL 3.4090 mL 6.8180 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (4.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (4.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.03%

SDS (251 KB)

COA (246 KB) HNMR (515 KB) RP-HPLC (149 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4090 mL 17.0451 mL 34.0901 mL 85.2253 mL
5 mM 0.6818 mL 3.4090 mL 6.8180 mL 17.0451 mL
10 mM 0.3409 mL 1.7045 mL 3.4090 mL 8.5225 mL
15 mM 0.2273 mL 1.1363 mL 2.2727 mL 5.6817 mL
20 mM 0.1705 mL 0.8523 mL 1.7045 mL 4.2613 mL
25 mM 0.1364 mL 0.6818 mL 1.3636 mL 3.4090 mL
30 mM 0.1136 mL 0.5682 mL 1.1363 mL 2.8408 mL
40 mM 0.0852 mL 0.4261 mL 0.8523 mL 2.1306 mL
50 mM 0.0682 mL 0.3409 mL 0.6818 mL 1.7045 mL
60 mM 0.0568 mL 0.2841 mL 0.5682 mL 1.4204 mL
80 mM 0.0426 mL 0.2131 mL 0.4261 mL 1.0653 mL
100 mM 0.0341 mL 0.1705 mL 0.3409 mL 0.8523 mL
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HA-1004 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HA-100491742-10-8HA1004HA 1004PKACyclic GMP-AMP SynthaseERKCalcium ChannelProtein kinase AcGASExtracellular signal regulated kinasesCa2+ channelsCa channelsMAPKheartmorphine withdrawaltyrosine hydroxylaseInhibitorinhibitorinhibit

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