1. GPCR/G Protein
  2. Adenylate Cyclase
  3. NKH477

NKH477  (Synonyms: Colforsin dapropate hydrochloride)

Cat. No.: HY-103193 Purity: 99.86%
COA Handling Instructions

NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.

For research use only. We do not sell to patients.

NKH477 Chemical Structure

NKH477 Chemical Structure

CAS No. : 138605-00-2

Size Price Stock Quantity
1 mg USD 40 In-stock
5 mg USD 100 In-stock
10 mg USD 180 In-stock
25 mg USD 380 In-stock
50 mg USD 650 In-stock
100 mg USD 1050 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts[1].

IC50 & Target

Adenylate Cyclase[1]

In Vivo

NKH477 (Colforsin dapropate hydrochloride) (orally; 1-3 mg/kg/day; days 3 and 5) prolonged lung allograft survival in a dose dependent manner[1].

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

Animal Model: Specific-pathogen-free inbred male Lewis rats (LEW) weighing 250 to 280 g[1]
Dosage: 1, 2 or 3 mg/kg/day
Administration: Orally; daily; Days 3 and 5
Result: Prolonged lung allograft survival in a dose dependent manner.
Molecular Weight

546.09

Formula

C27H44ClNO8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]12[C@@]3([C@@](C(C)(CC[C@@H]3O)C)([H])[C@H](OC(CCN(C)C)=O)[C@H](OC(C)=O)[C@]1(O[C@](C=C)(C)CC2=O)C)C.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (183.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (36.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8312 mL 9.1560 mL 18.3120 mL
5 mM 0.3662 mL 1.8312 mL 3.6624 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 5 mg/mL (9.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.86%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.8312 mL 9.1560 mL 18.3120 mL 45.7800 mL
5 mM 0.3662 mL 1.8312 mL 3.6624 mL 9.1560 mL
10 mM 0.1831 mL 0.9156 mL 1.8312 mL 4.5780 mL
15 mM 0.1221 mL 0.6104 mL 1.2208 mL 3.0520 mL
20 mM 0.0916 mL 0.4578 mL 0.9156 mL 2.2890 mL
25 mM 0.0732 mL 0.3662 mL 0.7325 mL 1.8312 mL
30 mM 0.0610 mL 0.3052 mL 0.6104 mL 1.5260 mL
DMSO 40 mM 0.0458 mL 0.2289 mL 0.4578 mL 1.1445 mL
50 mM 0.0366 mL 0.1831 mL 0.3662 mL 0.9156 mL
60 mM 0.0305 mL 0.1526 mL 0.3052 mL 0.7630 mL
80 mM 0.0229 mL 0.1144 mL 0.2289 mL 0.5722 mL
100 mM 0.0183 mL 0.0916 mL 0.1831 mL 0.4578 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Product Name:
NKH477
Cat. No.:
HY-103193
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