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

MedKoo CAT#: 319650

CAS#: 1762-34-1

Description: Abametapir is the active ingredient of Xeglyze Lotion. Abametapir inhibits metalloproteinases; enzymes that are essential to physiological processes critical for egg development and the survival of nymph and adult lice. In vitro and ex vivo research has demonstrated that abametapir not only kills the lice, but also prevents hatching of their eggs. Xeglyze Lotion is emerging as a differentiated development candidate to treat head lice infestations.


Chemical Structure

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Abametapir
CAS# 1762-34-1

Theoretical Analysis

MedKoo Cat#: 319650
Name: Abametapir
CAS#: 1762-34-1
Chemical Formula: C12H12N2
Exact Mass: 184.10
Molecular Weight: 184.242
Elemental Analysis: C, 78.23; H, 6.57; N, 15.21

Price and Availability

Size Price Availability Quantity
1g USD 90 Ready to ship
2g USD 150 Ready to ship
5g USD 250 Ready to ship
10g USD 425 Ready to ship
25g USD 750 2 Weeks
50g USD 1150 2 Weeks
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Synonym: HA-44; HA44; HA 44; BRN 0123183; BRN-0123183; BRN0123183; Abametapir; Xeglyze; 6,6'-Bi-3-picoline

IUPAC/Chemical Name: 5,5'-dimethyl-2,2'-bipyridinyl

InChi Key: PTRATZCAGVBFIQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H12N2/c1-9-3-5-11(13-7-9)12-6-4-10(2)8-14-12/h3-8H,1-2H3

SMILES Code: CC1=CN=C(C2=NC=C(C)C=C2)C=C1

Appearance: White to off-white solidw powder

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: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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:

Product Data:
Safety Data Sheet (SDS):
Biological target: Abametapir is a metalloproteinase (MMP) inhibitor.
In vitro activity: Treatment of head louse eggs with abametapir (0.74% in isopropanol) resulted in complete inhibition of hatching (100% ovicidal) in all stages of egg development from Day 0 to Day 8 (Table 1). At 0.55% abametapir, approximately 5.4% of the 6–8-d-old eggs hatched, in contrast to none of the 0–2- and 3–5-d-old eggs. As the concentration of abametapir declined, egg hatch increased in a concentration-dependent manner. A statistically significant concentration-dependent response was observed for all egg stages, with younger eggs (0–2 d) proving to be the most susceptible (LC50 = 0.108 (0.079–0.13) % abametapir concentration), followed by the 3–5-d-old eggs (LC50 = 0.121 (0.093-0.146) % abametapir concentration), whereas the oldest aged eggs (6–8 d) were most refractory to the treatment (LC50 = 0.160 (0.147–0.174) % abametapir concentration; Fig 1). Reference: J Med Entomol. 2017 Jan; 54(1): 167–172. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5853637/
In vivo activity: N/A

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.5 127.55
DMF 15.0 81.41
Ethanol 15.0 81.41
Ethanol:PBS (pH 7.2) (1:4) 0.2 1.09

Preparing Stock Solutions

The following data is based on the product molecular weight 184.24 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: 1. Bowles VM, Yoon KS, Barker SC, Tran C, Rhodes C, Clark MJ. Ovicidal Efficacy of Abametapir Against Eggs of Human Head and Body Lice (Anoplura: Pediculidae). J Med Entomol. 2017 Jan;54(1):167-172. doi: 10.1093/jme/tjw132. Epub 2016 Aug 21. Erratum in: J Med Entomol. 2017 Jan 1;54(1):248. PMID: 28082644; PMCID: PMC5853637.
In vitro protocol: N/A
In vivo protocol: 1. Bowles VM, Yoon KS, Barker SC, Tran C, Rhodes C, Clark MJ. Ovicidal Efficacy of Abametapir Against Eggs of Human Head and Body Lice (Anoplura: Pediculidae). J Med Entomol. 2017 Jan;54(1):167-172. doi: 10.1093/jme/tjw132. Epub 2016 Aug 21. Erratum in: J Med Entomol. 2017 Jan 1;54(1):248. PMID: 28082644; PMCID: PMC5853637.

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1: Woods AD, Porter CL, Feldman SR. Abametapir for the Treatment of Head Lice: A Drug Review. Ann Pharmacother. 2022 Mar;56(3):352-357. doi: 10.1177/10600280211027968. Epub 2021 Jun 22. PMID: 34157881.


2: Sunder M. Abametapir 0.74% (Xeglyze) for the Treatment of Head Lice. Am Fam Physician. 2022 Jul;106(1):91-92. PMID: 35839355.


3: Ogbuefi N, Kenner-Bell B. Common pediatric infestations: update on diagnosis and treatment of scabies, head lice, and bed bugs. Curr Opin Pediatr. 2021 Aug 1;33(4):410-415. doi: 10.1097/MOP.0000000000001031. PMID: 34074914.


4: Bowles VM, VanLuvanee LJ, Alsop H, Hazan L, Shepherd K, Sidgiddi S, Allenby K, Ahveninen T, Hanegraaf S. Clinical studies evaluating abametapir lotion, 0.74%, for the treatment of head louse infestation. Pediatr Dermatol. 2018 Sep;35(5):616-621. doi: 10.1111/pde.13612. Epub 2018 Jul 12. PMID: 29999197; PMCID: PMC6175393.


5: Bowles VM, Yoon KS, Barker SC, Tran C, Rhodes C, Clark MJ. Ovicidal Efficacy of Abametapir Against Eggs of Human Head and Body Lice (Anoplura: Pediculidae). J Med Entomol. 2017 Jan;54(1):167-172. doi: 10.1093/jme/tjw132. Epub 2016 Aug 21. Erratum in: J Med Entomol. 2017 Jan 1;54(1):248. PMID: 28082644; PMCID: PMC5853637.


6: Bowles VM, Hanegraaf S, Ahveninen T, Sidgiddi S, Allenby K, Alsop H. Effect of a New Head Lice Treatment, Abametapir Lotion, 0.74%, on Louse Eggs: A Randomized, Double-Blind Study. Glob Pediatr Health. 2019 Feb 22;6:2333794X19831295. doi: 10.1177/2333794X19831295. PMID: 30828591; PMCID: PMC6388454.


7: Taylor S, Walther D, Fernando DD, Swe-Kay P, Fischer K. Investigating the Antibacterial Properties of Prospective Scabicides. Biomedicines. 2022 Dec 19;10(12):3287. doi: 10.3390/biomedicines10123287. PMID: 36552044; PMCID: PMC9776028.


8: Clark JM. New chemistries for the control of human head lice, Pediculus humanus capitis: A mini-review. Pestic Biochem Physiol. 2022 Feb;181:105013. doi: 10.1016/j.pestbp.2021.105013. Epub 2021 Dec 16. PMID: 35082036; PMCID: PMC8795694.