MedKoo Cat#: 556156 | Name: Lonodelestat

Description:

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

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

Lonodelestat
Lonodelestat
CAS#906547-89-5

Theoretical Analysis

MedKoo Cat#: 556156

Name: Lonodelestat

CAS#: 906547-89-5

Chemical Formula: C71H111N15O19

Exact Mass: 1477.8181

Molecular Weight: 1478.76

Elemental Analysis: C, 57.67; H, 7.57; N, 14.21; O, 20.56

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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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.

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
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.