2. Metabolic Enzyme/Protease
  3. Procollagen C Proteinase
  4. UK-383367

UK-383367 is an orally available pro-collagen C-protease inhibitor (BMP-1) with an IC50 value of 44 nM. UK-383367 can reduce renal fibrosis and inflammation in chronic kidney disease (CKD) and may be used to study postoperative skin scarring.

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

UK-383367 Chemical Structure

UK-383367 Chemical Structure

CAS No. : 348622-88-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 120 In-stock
10 mg USD 200 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

UK-383367 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

UK-383367 is an orally available pro-collagen C-protease inhibitor (BMP-1) with an IC50 value of 44 nM. UK-383367 can reduce renal fibrosis and inflammation in chronic kidney disease (CKD) and may be used to study postoperative skin scarring[1][2][3].

In Vitro

UK-383367 (100-1000 nM, 24 h) inhibits the activity of NRK-49F cells[1].
UK-383367 (100-200 nM, 30 min) effectively suppresses the fibrotic response induced by TGF-β1 in mPTCs cells and shows a direct anti-fibrotic effect on renal cells in NRK-49F cells[1].

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

UK-383367 Related Antibodies

Cell Viability Assay[1]

Cell Line: mPTCs induced by TGF-β
Concentration: 0, 100, 200, 300, 400, 800, 1000 nM
Incubation Time: 24 h
Result: Inhibited cell proliferation.

Western Blot Analysis[1]

Cell Line: mPTCs induced by TGF-β, NRK-49F
Concentration: 100, 200 nM
Incubation Time: 30 min
Result: Inhibited the induction of collagen I/III, fibronectin, and α-SMA in cells, blocked the activation of NRK-49F cells, and blocked the activation of NRK-49F renal fibroblasts.
In Vivo

UK-383367 (5 mg/kg, intraperitoneal injection, once daily for seven days) improves tubulointerstitial fibrosis and inflammation in unilateral ureteral obstruction (UUO) chronic kidney disease (CKD) mice[1].
Pharmacokinetics of single intravenous and oral administration in rats and dogs[2]

Animal Intravenous dose (mg/kg) Elimination half-life (h) Plasma clearance (mL/min•kg) Volume of distribution (1/kg) Oral dose (mg/kg) Cmax (ng/mL) Tmax (h) Oral bioavailability (%)
Male rat 2.0 0.8 157 12.0 / / / /
Male dog 0.5 1.5 35 4.6 2 110 0.5-1.5 13

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

Animal Model: Unilateral Ureteral Obstruction (UUO) CKD mouse model[1]
Dosage: 5 mg/kg, daily, 7 days
Administration: Intraperitoneal injection (i.p.)
Result: Improved the fibrosis in small ducts, reduced the deposition of collagen I, collagen III, and fibronectin (FN), and it suppressed the upregulation of α-SMA, lessening the expression of the inflammatory markers IL-1β and MCP1.
Molecular Weight

324.38

Formula

C15H24N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(C1=NOC([C@H](CCCC2CCCCC2)CC(NO)=O)=N1)=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 : 65 mg/mL (200.38 mM; Need ultrasonic and warming; 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 3.0828 mL 15.4140 mL 30.8280 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (7.71 mM); 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.71 mM); 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:

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: 99.92%

COA (249 KB) HNMR (114 KB) RP-HPLC (178 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 3.0828 mL 15.4140 mL 30.8280 mL 77.0701 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 mL 15.4140 mL
10 mM 0.3083 mL 1.5414 mL 3.0828 mL 7.7070 mL
15 mM 0.2055 mL 1.0276 mL 2.0552 mL 5.1380 mL
20 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8535 mL
25 mM 0.1233 mL 0.6166 mL 1.2331 mL 3.0828 mL
30 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5690 mL
40 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
50 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
60 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
80 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
100 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
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UK-383367 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:

UK-383367348622-88-8UK383367UK 383367Procollagen C ProteinaseSkin scarringanti-inflammatoryrenal fibrosisInhibitorinhibitorinhibit

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