1. Metabolic Enzyme/Protease
  2. Elastase
  3. DMP 777

DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

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

DMP 777 Chemical Structure

DMP 777 Chemical Structure

CAS No. : 157341-41-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 248 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

IC50 & Target

Human leukocyte elastase (HLE)[2]

In Vivo

DMP-777-treated rats show a marked decrease in H/K-ATPase staining parietal cells. DMP-777-induced loss of parietal cells is significantly ameliorated with coadministration of omeprazole. DMP-777-treated animals demonstrates marked foveolar hyperplasia in the fundus with prominent expansion of diastase-resistant, PAS-positive surface mucous cells. When DMP-777 is coadministered with omprazole, there is a significant decrease in BrdUpositive S-phase cells compared with rats thatreceive DMP-777 alone[1]. After oral dosing of monkeys at 40 mg/kg with DMP-777 the only stereoisomer detected in the post-dose plasma samples is the starting material DMP-777, and no inversion of the configuration at positions 'a' and 'b' of DMP-777 has occurred in vivo[2]. Mist1-/- mice treated with DMP-777 show fewer chief cell to SPEM transitions. Mist1-/- mice treated with L635 demonstrates significantly fewer proliferative SPEM cells compared to control mice[3].

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

Molecular Weight

564.67

Formula

C31H40N4O6

CAS No.
Appearance

Solid

SMILES

CCC[C@H](C1=CC2=C(C=C1)OCO2)NC(N3[C@H](C(CC)(C3=O)CC)OC4=CC=C(C=C4)C(N5CCN(CC5)C)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 38.33 mg/mL (67.88 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 1.7709 mL 8.8547 mL 17.7095 mL
5 mM 0.3542 mL 1.7709 mL 3.5419 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 (stored under nitrogen). 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

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Volume (start)

V1

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Concentration (final)

C2

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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:  15% Cremophor EL    85% Saline

    Solubility: 35 mg/mL (61.98 mM); Suspended solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.43 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.75%

References
Animal Administration
[1]

Groups 1A and 1B receive control vehicle instead of omeprazole and DMP-777. Group 2A and 2B are dosed with DMP-777 once daily on Study Day 3 or Days 3 and 4, respectively, and receive control vehicle instead of omeprazole. Groups 3A and 3B are treated with omeprazole twice daily on Study Days 1 to 3 or Days 1 to 4, respectively, and receive control vehicle instead of DMP-777. Groups 4A and 4B are dosed with both omeprazole and DMP-777. On Study Days 1 and 2, animals are pretreated with omeprazole twice daily, the dosing intervals separated by approximately 6 hr. On Study Day 3 (Group 4A) or Days 3 and 4 (Group 4B), omeprazole is coadministered with DMP-777. The first dose of omeprazole is administered approximately 1 hr prior to the dose of DMP-777. The second dose is approximately 6 hr after the last dose of DMP-777. Groups 1A, 2A, 3A, and 4A are sacrificed on Day 4. Groups 1B, 2B, 3B, and 4B are sacrificed on Day 5. Bromodeoxyuridine (BrdU) is administered by intraperitoneal injection to all the rats, 2 hr prior to necropsy.

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

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 (stored under nitrogen). 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 1.7709 mL 8.8547 mL 17.7095 mL 44.2736 mL
5 mM 0.3542 mL 1.7709 mL 3.5419 mL 8.8547 mL
10 mM 0.1771 mL 0.8855 mL 1.7709 mL 4.4274 mL
15 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9516 mL
20 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2137 mL
25 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 mL
30 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
40 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1068 mL
50 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
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DMP 777 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.

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