U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 231 - 240 of 4716 results

Menthyl lactate is derived from menthol, a compound that comes from peppermint oil, or is made synthetically. Menthol has a natural cooling effect, which makes it useful as a topical analgesic to treat skin irritation, pain, itching or sunburn. Despite its cooling benefits, menthol can be a skin irritant. Like menthol, menthyl lactate is cooling, but it causes less skin irritation than menthol. Menthyl lactate also has a refreshing, minty taste. For this reason, some manufacturers use it as a flavoring ingredient. The compound is recommended for use as a flavor in concentrations of 0.005% to 0.2% and in cosmetic and other external products in concentrations ranging from 0.2% to 2.0%. Menthyl lactate is a known compound available e.g. from Haarmann & Reimer GmbH (Germany) under the name FRESCOLAT, Type ML.
Resorcinol is a benzenediol. Resorcinol is commonly used in hair dyes and acne medication. Resorcinol works by breaking down rough, scaly, or hardened skin. Resorcinol also disinfects the skin to help fight infection. Resorcinol topical (for the skin) is used to treat pain and itching caused by minor cuts and scrapes, burns, insect bites, poison ivy, sunburn, or other skin irritations. Resorcinol topical is also used to treat acne, eczema, psoriasis, seborrhea, corns, calluses, warts, and other skin disorders. Resorcinol is included in the FDA final rule list of all permitted active ingredients for OTC topical acne products. Permitted combination active ingredient product - Resorcinol in 2 percent concentration in combination with sulfur in concentrations of between 3 and 8 percent. In oxidative hair dyes, resorcinol is regulated to 5% or below in practice, however, many manufacturers limit the level of free resorcinol in oxidative hair dyes to 1.25%. Resorcinol is limited to 0.5% in shampoos and hair lotions. Resorcinol is usually present in anti-acne preparations at a maximum concentration of 2%. The concentration of resorcinol can be much higher in peels, in some cases around 50%. Jessner’s solution (resorcinol in ethyl alcohol, 14% w/v; lactic acid, 14%; and salicylic acid, 14%) is commonly used in chemical peeling. A specialized medical use of resorcinol is in biological glues (gelatin–resorcinol–formaldehyde glue) for cardiovascular surgery, in particular aortic operations.
Status:
US Approved OTC
Source:
21 CFR 358.710(b)(4) dandruff:seborrheic dermatitis salicylic acid
Source URL:
First marketed in 1860
Source:
sodium salicylate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Methyl salicylate (or methyl 2-hydroxybenzoate), also known as wintergreen oil, is a natural product and is present in white wine, tea, porcini mushroom Boletus edulis, Bourbon vanilla, clary sage, red sage and fruits including cherry, apple, raspberry, papaya and plum. Methyl salicylate is topically used in combination with methanol and under brand name SALONPAS to temporarily relieves mild to moderate aches and pains of muscles and joints associated with: strains, sprains, simple backache, arthritis, bruises. The precise mechanism of action of methyl salicylate is not known, but there is suggested, that it cause dilation of the capillaries thereby increasing blood flow to the area.
Status:
Investigational
Source:
INN:cambritaxestat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02444910: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:zoldonrasib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00598806: Phase 3 Interventional Completed Bladder Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Apaziquone (EOquin, EO9) is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases (such as NQO1). The active metabolites alkylate DNA and lead to apoptosis. In animal tumour models, EO9 was inactive against the P388 murine leukaemia but exhibited anti-tumour activity against human tumour xenografts and the generally chemo-resistant murine adenocarcinomas of the colon (MAC) tumours. Initial evidence that in vivo response correlated with NQO1 activity. Apaziquone was selected for clinical evaluation based upon its novel mechanism of action (which was distinct from MMC), its preferential activity against cells derived from solid tumours in vitro and in vivo, its ability to target both aerobic and hypoxic cells and the lack of myelosuppression in mice and rats. Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan, Inc. for the treatment of superficial (non-muscle invasive) bladder cancer. However, the US-FDA determined that it was not statistically effective.
Status:
Investigational
Source:
INN:carafiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carafiban is orally active heterocyclic peptide mimetics fibrinogen IIb/IIIa receptor antagonist with antithrombotic activity. Carafiban is a prodrug, that underwent metabolic transformation to active metabolite des-ethyl- Carafiban, that inhibited dose-dependently and reversibly human platelet aggregation. In conscious dogs, Carafiban showed a high plasma availability of the active moiety of 42±8% and a plasma half-life of 9.9 h after oral administration as measured by bioassay. Carafiban may potentially be used for chronic treatment and prophylaxis of thrombotic diseases in humans.
Status:
Investigational
Source:
NCT00280631: Phase 1/Phase 2 Interventional Completed Myelodysplastic Syndrome (MDS)
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ezatiostat (TLK199) [γ-glutamyl-S-(benzyl)cysteinyl-R-phenyl glycine diethyl ester] is an inhibitor of Glutathione S-transferase P1–1 (GSTπ). The drug is a peptidomimetic of GSH (glutathione), esterified to enhance cellular uptake and designed to bind to the “G-site” of GSTP1–1. Independent of catalysis inhibition, TLK199 also disrupts the protein:protein interaction site(s) between GSTP1–1 and JNK1. Telik Inc was developing TLK-199 for the potential prevention of myelosuppression in blood diseases, namely myelodysplastic syndrome.
Status:
Investigational
Source:
INN:elironrasib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)