Art. -Nr.: HY-13102

UK-383367

Name: UK-383367
Brand: MedChemExpress
SKU: HY-13102
Price: 100.00 USD
Availability: InStock
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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.

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Reinheit: 99.95%
CAS. Nr.: 348622-88-8
Formel: C₁₅H₂₄N₄O₄
Molecular Weight:324.38

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

UK-383367 Chemical Structure

CAS. Nr.: 348622-88-8

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	44 nM Compound: 7, UK-383367	Inhibition of human procollagen C-proteinase expressed in CHO cells by fluorescence assay Inhibition of human procollagen C-proteinase expressed in CHO cells by fluorescence assay	[PMID: 18945617]
CHO	IC₅₀	44 nM Compound: 1	Inhibition of human procollagen C-proteinase expressed in CHO cells Inhibition of human procollagen C-proteinase expressed in CHO cells	[PMID: 17591762]
Fibroblast	IC₅₀	2100 nM Compound: 7, UK-383367	Reduction in collagen deposition in human fibroblasts after 8 days by HPLC Reduction in collagen deposition in human fibroblasts after 8 days by HPLC	[PMID: 18945617]

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.

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)	C_max (ng/mL)	T_max (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.

Chemical Information

CAS. Nr. 348622-88-8
Appearance Solid
Molecular Weight 324.38
Formel C₁₅H₂₄N₄O₄
Color White to off-white
SMILES

NC(C1=NOC([C@H](CCCC2CCCCC2)CC(NO)=O)=N1)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0828 mL

15.4140 mL

30.8280 mL

5 mM

0.6166 mL

3.0828 mL

6.1656 mL

10 mM

0.3083 mL

1.5414 mL

3.0828 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mi Bai, et al. BMP1 inhibitor UK383,367 attenuates renal fibrosis and inflammation in CKD. Am J Physiol Renal Physiol. 2019 Dec 1;317(6):F1430-F1438. [Content Brief]

[2]. Allan GA, et al. Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica. 2006 May;36(5):399-418. [Content Brief]

[3]. Eugenia C Salcedo, et al. Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer. ACS Chem Biol. 2021 Apr 16;16(4):712-723. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Keywords

Produktname:
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MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

UK-383367

SB 525334

NSC 405020

DMH-1

LDN193189

K02288

LDN193189 (GMP)

Acetyltetrapeptide 11

DMH-1 (Standard)

DMH-1 (GMP)

K02288 (GMP)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

UK-383367

SB 525334

NSC 405020

DMH-1

LDN193189

K02288

LDN193189 (GMP)

Acetyltetrapeptide 11

DMH-1 (Standard)

DMH-1 (GMP)

K02288 (GMP)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UK-383367 Related Classifications

HY-13102 Related Classifications

Bioz