Nocarnickelamide B TFA
Nocarnickelamide B TFA is a ROCK1/2 inhibitor with IC50 values of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B TFA inhibits the activation of ROCK-regulated cytoskeletal contraction markers (especially myosin light chain) in human trabecular meshwork cells. Nocarnickelamide B TFA can be used in the research of glaucoma.
For research use only. We do not sell to patients.
- Formula: C29H42N6O9·xC2HF3O2
- Molecular Weight:618.68 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ROCK1 14.9 μM (IC50) |
ROCK2 21.9 μM (IC50) |
In Vitro
Nocarnickelamide B (Compound 2) (10-30 μM; 6 h) TFA inhibits the phosphorylation of MYPT1 and MLC2, two cytoskeletal contraction markers regulated by ROCK, in human trabecular meshwork cells, without affecting the protein expression of ROCK1 or ROCK2[1].
Nocarnickelamide B (3-30 μM; 72 h) TFA enhances the permeability of TGF-β2-stimulated human trabecular meshwork cell monolayers in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human trabecular meshwork (HTM) cells
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Concentration:10, 30 μM
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Incubation Time:6 h
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Result:Significantly inhibited phosphorylation of MYPT1 (Thr696) and MLC2 (Thr18/Ser19), key markers of cytoskeletal contraction.
Did not alter total ROCK1 or ROCK2 protein expression levels.
Chemical Information
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Molecular Weight 618.68 (free base)
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Formula C29H42N6O9·xC2HF3O2
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SMILES
CC(C)C[C@@H](NC(CNC([C@H]1N(C([C@H](N)CC2=CC=CC=C2)=O)C[C@H](O)C1)=O)=O)C(N3C[C@H](O)C[C@H]3C(NCC(O)=O)=O)=O.OC(C(F)(F)F)=O.[x]
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Sequence
{DPhe}-Hyp-Gly-{DLeu}-Hyp-Gly
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Sequence Shortening
{DPhe}-Hyp-G-{DLeu}-Hyp-G
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nocarnickelamide B TFA Related Classifications
HY-N15301A Related Classifications
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