Lonodelestat

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 556156

CAS#: 906547-89-5

Description: Lonodelestat, also known as POL6014, is a potent, selective inhibitor of human neutrophil elastase (NE). Preclinical studies in animals demonstrated that the investigational NE inhibitor could reduce inflammatory markers and the number of neutrophils. POL6014 significantly improves RVP and attenuates right ventricular hypertrophy in a rat MCT-induced PAH model after chronic IT administration. POL6014 at 0.3 mg/kg is as efficient as Tadalafil at 10 mg/kg. The PEM NE inhibitor POL6014 may thus provide another therapeutic treatment option for PAH.

Chemical Structure

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Lonodelestat
CAS# 906547-89-5
Instruction

Theoretical Analysis

MedKoo Cat#: 556156
Name: Lonodelestat
CAS#: 906547-89-5
Chemical Formula: C71H111N15O19
Exact Mass: 1,477.82
Molecular Weight: 1,478.755
Elemental Analysis: C, 57.67; H, 7.57; N, 14.21; O, 20.56

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Lonodelestat; POL6014; POL-6014; POL 6014;

IUPAC/Chemical Name: Cyclo[L-alanyl-L-seryl-L-isoleucyl-L-prolyl-L-prolyl-L-glutaminyl-L-lysyl-L-tyrosyl-D-prolyl-L-prolyl-(2S)-2-aminodecanoyl-L-α-glutamyl-L-threonyl]

InChi Key: JMWYNUHGKFJVIB-QGFXQWJDSA-N

InChi Code: InChI=1S/C71H111N15O19/c1-6-8-9-10-11-12-19-46-60(94)76-48(30-32-56(91)92)63(97)82-58(42(5)88)67(101)74-41(4)59(93)80-50(39-87)64(98)81-57(40(3)7-2)71(105)86-37-18-24-54(86)70(104)84-35-16-22-52(84)66(100)78-47(29-31-55(73)90)62(96)75-45(20-13-14-33-72)61(95)79-49(38-43-25-27-44(89)28-26-43)68(102)85-36-17-23-53(85)69(103)83-34-15-21-51(83)65(99)77-46/h25-28,40-42,45-54,57-58,87-89H,6-24,29-39,72H2,1-5H3,(H2,73,90)(H,74,101)(H,75,96)(H,76,94)(H,77,99)(H,78,100)(H,79,95)(H,80,93)(H,81,98)(H,82,97)(H,91,92)/t40-,41-,42+,45-,46-,47-,48-,49-,50-,51-,52-,53+,54-,57-,58-/m0/s1

SMILES Code: O=C1[C@@]2(N(C(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@]4(N(C(=O)[C@]5(N(C(=O)[C@]([C@H](CC)C)(NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@]([C@@H](C)O)(NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCCCCC)NC(=O)[C@]6(N1CCC6)[H])[H])[H])CCC5)[H])CCC4)[H])CCC2)[H]

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Neutrophil elastase is an enzyme that plays an essential role in inflammation. When the lungs are infected with bacteria, white blood cells release enzymes, including neutrophil elastase, to fight the infection. In CF, these enzymes can result in excessive inflammation that causes damage to the lungs. Blocking the function of neutrophil elastase may minimize tissue destruction and decrease inflammation within the CF airway.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,478.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Weber AG, Chau AS, Egeblad M, Barnes BJ, Janowitz T. Nebulized in-line endotracheal dornase alfa and albuterol administered to mechanically ventilated COVID-19 patients: a case series. Mol Med. 2020 Sep 29;26(1):91. doi: 10.1186/s10020-020-00215-w. PMID: 32993479; PMCID: PMC7522910.


2: Weber AG, Chau AS, Egeblad M, Barnes BJ, Janowitz T. Nebulized in-line endotracheal dornase alfa and albuterol administered to mechanically ventilated COVID-19 patients: A case series. medRxiv [Preprint]. 2020 May 15:2020.05.13.20087734. doi: 10.1101/2020.05.13.20087734. Update in: Mol Med. 2020 Sep 29;26(1):91. PMID: 32511514; PMCID: PMC7273282.


3: Zuo Y, Yalavarthi S, Shi H, Gockman K, Zuo M, Madison JA, Blair C, Weber A, Barnes BJ, Egeblad M, Woods RJ, Kanthi Y, Knight JS. Neutrophil extracellular traps in COVID-19. JCI Insight. 2020 Jun 4;5(11):e138999. doi: 10.1172/jci.insight.138999. PMID: 32329756; PMCID: PMC7308057.


4: Barth P, Bruijnzeel P, Wach A, Sellier Kessler O, Hooftman L, Zimmermann J, Naue N, Huber B, Heimbeck I, Kappeler D, Timmer W, Chevalier E. Single dose escalation studies with inhaled POL6014, a potent novel selective reversible inhibitor of human neutrophil elastase, in healthy volunteers and subjects with cystic fibrosis. J Cyst Fibros. 2020 Mar;19(2):299-304. doi: 10.1016/j.jcf.2019.08.020. Epub 2019 Sep 6. PMID: 31501052.