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

DMP 777 (Synonyms: L-694458)

Cat. No.: HY-75957 Purity: 99.13%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 248 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
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10 mg USD 300 In-stock
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25 mg USD 510 In-stock
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50 mg USD 815 In-stock
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100 mg USD 1350 In-stock
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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].

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

Molecular Weight

564.67

Formula

C₃₁H₄₀N₄O₆

CAS No.

157341-41-8

SMILES

CCC[[email protected]](C1=CC2=C(C=C1)OCO2)NC(N3[[email protected]](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)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.1771 mL 0.8855 mL 1.7709 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

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

    Solubility: 2.5 mg/mL (4.43 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 99.13%

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Keywords:

DMP 777L-694458DMP777DMP-777L694458L 694458ElastaseInhibitorinhibitorinhibit

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